WP1 Staff exchange

Outgoing visits

1. Aiga Grandāne

Host institution: University of Florence, Italy

http://www.unifi.it
http://www2.chim.unifi.it

Aim: Acquirement of advanced methods for the design and synthesis of inhibitors of Zn-depending enzymes. The main attention was focused on carbonic anhydrases (CA) where the most interesting isoforms are CA IX and CA XII related to the cancer. Design and synthesis of coumarin bioisosteres as selective inhibitors of cancer related isoforms of CA was performed.

Results: As a main result of the visit is synthesized series of original inhibitors of CA for biological screening. Two manuscripts are in preparation. As a second result but not less important is indispensable experience of work organization in foreign laboratories. As a last result shell be mentioned strengthened collaboration between Latvian Institute of Organic Synthesis and University of Florence which in future will result in new projects.

Dates of visit: 01.10.2013-28.02.2014

Status: Implemented.

 

2. Edgars Paegle

Host institution: University of Lorraine in Metz (previously - University of Metz), France

http://www.srsmc.univ-lorraine.fr/spip3011/?-Presentation-&lang=fr
Aim: Development of a new potentially biologically active derivatives of thiophene and selenophene.

Results: Synthesis of new selenium analogues of raloxifene (Evista®), which is selective estrogen receptor modulator (SERM) used for treatment of osteoporosis in postmenopausal women and for prevention of breast cancer. The main goal of this research is to discover potential drugs for treatment of estrogen dependent cancers. New thiophene derivative of raloxifene’s selenium analogue was obtained during the visit.

Synthesis of new type of hypervalent T-shaped 10-Se-3 systems: Synthetic procedure for preparation of new type of hypervalent selenium compounds was elaborated and obtained results will be published in the near future.

Dates of visit: 04.11.2013-31.03.2014

Status: Implemented.

 

3. Mārtiņš Priede

Host institution: University of Jyväskylä, Finland

https://www.jyu.fi/kemia/tutkimus/orgaaninen/en/research/Pihko
https://www.jyu.fi/kemia/tutkimus/orgaaninen/en/research/Pihko/Group%20activities

Aim: Establish a collaboration program focused on the development of environmentally benign synthetic methodologies.

Results: Method development for substituted pyrrolidine; collaboration in total synthesis of Aspergillide A and B.

Dates of visit: 25.11.2013-25.04.2014

Status: Implemented.

 

4. Jekaterīna Ivanova

Host institution: University of Florence, Neurofarba Department, Section of Pharmaceutical Chemistry, Italy

http://www2.chim.unifi.it

Aim: The purpose of this visit was to get new experience in organic synthesis and work organization in foreign laboratory, develop methods for the design and synthesis of new potential anti-infective agents and enhance collaboration between LIOS and University of Florence.

Results: Advanced methods for the design and synthesis of anti-infective agents were acquired. Besides inherent experience on work organization, new and original series of potential Carbonic anhydrase (CA) inhibitors have been designed and synthesized for the CA inhibition studies.

The obtained results will be published. Two manuscripts are in preparation. Results also will be presented at international conferences and symposiums.
The outgoing visit will promote future collaboration between LIOS and University of Florence

Dates of visit: 03.02.2014-30.06.2014

Status: Implemented.

 

5. Signe Grinberga

Host institution: University of Copenhagen, Denmark
http://drug.ku.dk

Aim: Acquirement of advanced methods of structure-based drug design and synthesis.

Results: A series of 1-hydroxypyrazole based 4-PIOL analogues have been synthesized and characterized pharmacologically. The binding affinities of the compounds at native GABAA receptors were measured by displacement of [3H] muscimol in rat membrane preparations.

Dates of visit: 31.03.2014-30.08.2014

Status: Implemented.

 

6. Ilze Adlere

Host institution: UniversityLeiden, the Netherlands

http://medchem.leidenuniv.nl

Aim: Synthesis and evaluation of allosteric ligands of GPCR (adenosine A2A receptor).

Results: Acquired new methods for synthesis for GPCR (adenosine A2A receptor) ligands. Obtained final compounds Amiloride derivatives were submitted to biochemistry assays to test the binding affinity (IC50), displacement and dissociation rate of the antagonist radioligand on wild type and mutant adenosine A2A receptors and reveal the allosteric effect. Docking studies were performed to explain allosteric binding mode of the lead compound in A2A receptor binding pocket (in a collaboration with host group).

Dates of visit: 01.02.2014-30.06.2014

Status: Implemented.

 

7. Ilga Mutule

Host institution: Institüt für Organische Chemie, RWTH Aachen University, Germany.

http://bolm.oc.rwth-aachen.de

Aim: Establish a collaboration program focused on the development of iron and copper-catalyzed methodologies for functionalization of pharmaceutically relevant heterocycles.

Results: Investigation of sulfoximine arylation reactions using C-H activation approach have been studied in depth. Several transition metal catalysts (|Pd, Rh, Ru complexes) have been investigated to identify the most effective transition metal catalysts for these reactions.

Dates of visit: 02.01.2014-30.05.2014

Status: Implemented.

8. Anatolijs Mišņovs

Host institution:CRS4-Centre for advanced Studies, Research and development in Sardinia, Italy.

http://www.crs4.it/crs4/peopledetails/people/169/Detlef%20W.%20M._Hofmann

Aim: This experience exchange visit was aimed to obtaining the knowledge on the modern state in the field of crystal structure prediction for pharmaceutical crystalline substances by molecular mechanics and dynamics calculations. „In silico” screening of potential polymorfic forms, new crystalline forms and stable structures of multicomponent pharmaceutical solids is of great importance in pharmaceutical industry.

Results: Using the latest version of FlexCryst program suite for carrying out crystal structure prediction, crystal structure determination from X-ray powder diffraction data, calculation of thermodynamical properties, experimental structure optimization and crystal structure clustering studies of several pharmaceutically important molecules were carried out. Possible crystal structures are generated by placing molecules with varying positions and orientations into a unit cell of varying dimensions. FlexCryst software will be used at the Latvian Institute of Organic Synthesis.

Dates of visit: 02.05.2014-26.05.2014 and 01.06.2015-15.06.2015

Status: Implemented.

 

9. Iveta Luntēna

Host institution: Aalto University, Helsinki
http://users.tkk.fi/~akoskine
http://chemistry.aalto.fi/en/research/koskinen_group

Aim: Acquirement of advanced asymmetric synthetic methods of analogues of natural compounds - investigation and development of short and stereoselective synthetic sequence to decahydroisoquinoline frameworks utilizing amino acids as starting materials.

Results: During the research period scalable stereocontrolled synthesis of exo-methylene cyclization precursor was developed using Barbier reaction of amino aldehyde and allylic bromide. This also involved finding the optimal methods for decagram scale synthesis of precursors.

During the screening of various cyclization conditions (base mediated, radical mediated and transition metal mediated), the desired cyclization was finally achieved using iodine and base in aqueous THF. This mechanistically complex cyclization proceeds via several intermediates and allows obtaining the challenging anti-Markovnikov addition product. Thus the short 6 step sequence allows to generate significant molecular complexity (4 stereocenters, 2 fused rings) from simple and cheap starting materials. Importantly the configuration of the two unchangeable stereocenters of the model compound matches the configuration of the D-E-F core of steroidal alkaloids from Veratrum family.

Dates of visit: 01.05.2014-30.08.2014

Status: Implemented.

 

10. Andrejs Pelšs

Host institution: Aalto University, Helsinki
http://users.tkk.fi/~akoskine
http://chemistry.aalto.fi/en/research/koskinen_group

Aim: Acquirement of novel copper-catalysed methodologies for use in synthesis of natural compounds.

Results: Direct diastereodivergent one pot synthesis of amino epoxides from amino esters was developed. The previous synthesis of amino epoxides required three separate steps placed early in the synthetic sequence and performed on decagram scale. The newly developed one pot, one step methods significantly save time and effort and allow to execute the synthesis of amino epoxides in one pot and with either stereochemistry (syn or anti) simply by sequential addition of reagents in either order.

Dates of visit: 26.06.2014-29.08.2014

Status: Implemented.

 

11. Rufs Šmits

Host institution: University of Helsinki, Finland
http://www.helsinki.fi/biosciences/administration/biocenter2.htm

Aim: Acquirement of advanced methods for liposomal vesicle preparation and drug encapsulation.

Results: The size and zeta potential of liposomes obtained from cationic, amphyphilic compounds were determined.

Dates of visit: 02.06.2014-31.07.2014

Status: Implemented.

 

12. Marina Makrecka-Kūka

Host institution: Innsbruck Medical University, Austria

http://www.bioblast.at/index.php/Gnaiger_E

Aim: Learn advanced methods in experiments with mitochondria respiration

Results: The advanced methods to study mitochondrial function were learned and will be used in Latvian Institute of Organic Synthesis for screening and pharmacological characterization of drugs.

Dates of visit: 31.07.2014-01.10.2014.

Status: Implemented.

 

13. Mārtiņš Ruciņš

Host institution: Palacký University Olomouc, Czech Republic

http://ach.upol.cz/en/laborator-elektromigracnich-metod.php

Aim: Study and implementation of nanoparticles in capillary electrophoresis

Results: Capillary electrophoresis method (i.e. micellar electrokinetic chromatography) for analysis of several antiandrogenic drugs, as well as partition coefficients of model antiandrogenic drugs and some pesticides with STS micelles and asolectin liposomes were elaborated.

Dates of visit: 7.09.2014-06.02.2015.

Status: Implemented.

 

14. Diāna Borovika

Host institution: University „La Sapienza”, Rome, Italy

http://www.uniroma1.it/dottoratoscifarm

Aim: The synthesis of epigenetic enzyme inhibitors

Results: New series of novel nitrogen containing heterocyclic compounds incorporating both pyrolo and pyrazolo moieties have been designed and synthesised for DOT1L inhibition studies.

Dates of visit: 7.10.2014-06.03.2015.

Status: Implemented.

 

15. Anna Ņikitjuka

Host institution: Parma University Parma, Italy

http://old.unipr.it/arpa/dipfarm/medchem/index.htm

Aim: Studies of advanced methods of drug discovery

Results: During the experience exchange stay at Parma University in the group of prof. G. Costantino the synthesis of 1-benzyl-2-phenylcyclopropanecarboxylic acid bioisosters as a possible O-acetyl serine sulfhydrylase inhibitors was realized. Biological activity and lipophilicity have been evaluated for the new obtained final compounds

Dates of visit: 01.02.2015-01.05.2015.

Status: Implemented.

 

16. Kristaps Jaudzems

Host institution: Centre de RMN à Très Hauts Champs, Ecole Normale Supérieure de Lyon, France

http://www.ens-lyon.fr/crmn/crmn/index.html

Aim: NMR studies of biomedically relevant proteins and protein ligand complexes.

Results: Preliminary characterization of 13C and 15N labelled artificial spider silk by solid-state NMR.

Dates of visit: 27.04.2015-08.05.2015.

Status: Implemented.

 

17. Ilze Kumpiņa

Host institution: Uppsala University, BMC, Sweden

http://www.uu.se/enhttp://www.orgfarm.uu.se/

Aim: Develop microwave flow methodologies for synthesis of new angiotensin II AT2 receptor antagonists

Results: Developed a microwave promoted - continuous flow method for transcarbamylation of sulfonylcarbamates. A series of novel model alkyl (arylsulfonyl)carbamates as angiotensin II type 2 receptor ligands were synthesised by applying new reaction protocol.

Dates of visit: 03.05.2015-03.10.2015.

Status: Implemented.

 

18. Jānis Peļšs

Host institution: Laboratory of Organic Chemistry, Wageningen University, The Netherlands

http://www.wageningenur.nl/en/Expertise-Services/Chair-groups/Agrotechnology-and-Food-Sciences/Laboratory-of-Organic-Chemistry.htm

Aim: to obtain skills on modern design, synthesis and preparation of self-organizing systems

Results: New polymeric materials combining the use of dynamic covalent bonds and metal-ligand interactions were designed, synthesized and characterized. Experience in work organization, and design, synthesis and preparation of self-organizing systems was acquired.

Dates of visit: 03.08.2015-30.12.2015.

Status: Implemented.

 

19. Gints Šmits

Host institution: Ecole Polytechnique Fédérale de Lausanne (EPFL), Switzerland

Aim: Gathering expertise in development of asymmetric metal-catalyzed methodologiesResults: A transition metal catalyzed C-C bond cleavage reactions were investigated. As a result new method for the synthesis of transition metal complexes was discovered. The newly developed approach is applicable for synthesis of chiral Rh and Ir catalysts further used for number of asymmetric reactions.

Dates of visit: 02.08.2015-31.12.2015.

Status: Implemented.

 

20. Dace Rasiņa

Host institution: Perugia University, Italy

http://www.chm.unipg.it/greensoc

Aim: Studies of green chemistry approaches in organic chemistry

Results: We have developed the Catellani reaction catalyzed by a heterogeneous palladium species in a renewable biomass-derived solvent (γ-valerolactone). The reaction works efficiently on a variety of alkenes, however the scope of aryl iodides is limited. The nature of the catalytically active species has been investigated, suggesting that the process is actually catalyzed by the heterogeneous catalyst when Pd/Al203 is used.

Dates of visit: 31.08.2014-29.01.2016.

Status: Implemented.

 

21. Mārtiņš Otikovs

Host institution: Centre de RMN à Très Hauts Champs, Ecole Normale Supérieure de Lyon, France

http://www.ens-lyon.fr/crmn/crmn/index.html

Aim: NMR studies of artificially produced spider silk

Results: During the visit solid state NMR spectra under ultra-fast (60 kHz) magic angle spinning of artificially produced spider silk were acquired and analyzed.

Dates of visit: 19.10.2015-18.12.2015.

Status: Implemented.

 

22. Diāna Zeļencova

Host institution: Host institution: Department of Biochemistry, University of Zürich, Switherland
http://www.biochem-caflisch.uzh.ch/

Aim: Obtaining expertise in computational studies of metaloproteins

Results: During the experience exchange stay in the group of prof. A. Caflisch the methods and protocols for explicit solvent molecular dynamics simulations of metaloproteins were learned. As well as, the insights into the new approach for structure based molecular docking was gained.

Dates of visit: 15.09.2015-12.12.2015.

Status: Implemented.

 

23. Vitālijs Romanovs

Host institution: University of Rennes 1, Rennes, France

https://perso.univ-rennes1.fr/viatcheslav.jouikov/

Aim: Coordination of synthetic efforts aiming redox active and spin-switching biologically active organosilicon derivatives

Results: First axes: The comparison with model systems proved the feasibility and a great promise of these new PàM hypercoordinated derivatives. Second axes: New family of triptych silatranes has been elaborated. Third axes: This is a first example of the covalent attachment of an electro- commutable spin marker to the solid carbon support in a one-step non-diazonium process using a simple and flexible methylene linker.

Dates of visit: 03.09.2015-06.12.2015.

Status: Implemented.

 

24. Jānis Kūka

Host institution: Jagellonian Centre for Experimental Therapeutics, Jagellonian University, Krakow, Poland

http://jcet.eu/en/

Aim: Participation in the studies of isolated heart model, endothelial toxicity studies and functionality assays

Results: During the visit improved techniques to work with isolated mouse heart, particularly Langendorff model, were learned and will be used in studies to find novel targets for cardioprotection in LIOS. Endothelium toxicity studies and functionality assays were performed in endothelial cell culture to study and compare potential toxic effects of different acylcarnitines and pharmacological means to prevent acylcarnitine-induced mitochondrial- and cyto-toxicity. Endothelial cell culture was brought back to Riga and introduced in Laboratory of Pharmaceutical Pharmacology.

Dates of visit: 07.09.2015-07.10.2015.

Status: Implemented.

 

25. Olga Konstantinova

Host institution: Aalto University, Helsinki
http://users.tkk.fi/~akoskine
http://chemistry.aalto.fi/en/research/koskinen_group

Aim: Elaboration of new enantioselective methodologies for use in the synthesis of natural compounds

Results: A methodology to the synthesis of the fragment of calyculin C has been elaborated. Several building blocks of this fragment were synthesised during this period.

Dates of visit: 30.09.2015-01.03.2016.

Status: Implemented.

 

26. Līga Zvejniece

Host institution: University of Tartu, Biomedicum, Department of Pharmacology, Estonia

http://www.biomeditsiin.ut.ee/en/departments/department-pharmacology-0

Aim: Participation in studies of experimental behaviour models for applied research

Results: Promising preliminary data in pilot study about the role of neuropathic pain involvement in depression-like state in mice were obtained.

Dates of visit: 06.09.2015-03.10.2015.

Status: Implemented.

 

27. Reinis Vilšķērsts

Host institution: Jagellonian Centre for Experimental Therapeutics, Jagellonian University, Krakow, Poland

http://jcet.eu/en/

Aim: Participation in the studies of isolated mice aortic rings, studying deleterious effects of palmitoylcarnitine on functions of vascular endothelium and smooth muscle cells.

Results: During the visit the isolation and assessment of functionality of smooth muscle and endothelium of mice aortic rings were learned. Results from the experiments with palmitoylcarnitine revealed that co-incubation of aortic rings with palmitoylcarnitine induced marked endothelial dysfunction but had no effect on the functioning of vascular smooth muscle cells. Further, learned techniques will be used in LIOS for studying vasoprotective effects and mechanisms of newly synthesised compounds.

Dates of visit: 04.10.2015-04.11.2015.

Status: Implemented.

 

28. Diāna Borovika

Host institution: Leibniz Institute for Catalysis, at the University of Rostock, Germany

http://www.uniroma1.it/dottoratoscifarm

Aim: Advanced synthetic methods for sulfonyl groups introduction in aromatic and heteroaromatic compounds

Results: Novel heterogeneous cobalt containing catalyst which was characterized and applied in the catalytic hydrogenation of nitriles to corresponding primary amines. The catalyst exhibited high catalytic activity for a broad scope of aromatic, aliphatic and heterocyclic nitriles which contain different functional groups.​

Dates of visit: 12.10.2015-12.03.2016.

Status: Implemented.

 

29. Jekaterīna Ivanova

Host institution: Laboratory of Organic Chemistry, Wageningen University, The Netherlands

Aim: application of enzymes as selective, environmentally friendly catalysts in organic synthesis.

Results: Besides inherent experience on work organization, a number of aziridine derivatives were synthesized during the visit. Enzymatic catalysis was applied for the synthesis of the target compounds. Obtained aziridine derivatives were evaluated as novel tools for the immobilization of enzymes.

Dates of visit: 01.12.2015-30.04.2016.

Status: Implemented.

 

30. Anete Parkova

Host institution: University of Oxford, Oxford, UK

Aim: Development of new methods for synthesis of small nitrogen heterocycles

Results: During this visit to Chemistry Research Laboratory, Department of Chemistry, University of Oxford Bell protein protein production and purification have been performed. A synthesis of six membered boronic acid derivatives have been carried out. A suitable protecting group, convenient method for synthesis of boronate derivative with pinanediol boronic ester, and suitable conditions for Matteson's boronic ester homologation have been also found.

Dates of visit: 16.11.2015-16.04.2016.

Status: Implemented.

 

31. Dmitrijs Stepanovs

Host institution: University of Oxford, Oxford, UK

Aim: Studies of systems and techniques relevant to macromolecular crystallography and its applications

Results: In order to achieve the aim of the programme, the work in University of Oxford included theoretical background and practice in macromolecular crystallography:

  1. Crystal growth of macromolecules;
  2. Crystal structure determination using CrystClear, GDA, ISpyB, HKL2000, Phenix, WinCoot and other software;
  3. Crystal structure analysis and deposition;
  4. Eight crystal structures of ligand/biomolecule complexes have been determined during the visit.

Dates of visit: 30.11.2015-30.04.2016.

Status: Implemented.

 

32. Inguna Goba

Host institution: Helmholtz Zentrum München (Technische Universität München), Germany

Aim: Studies of membrane protein expression, technology of nanodiscs, membrane protein incorporation in nanodiscs, NMR and ITC studies of membrane proteins and protein-ligand complexes

Results: During the research visit cloning, bacterial expression and chromatographic purification of Sigma-1 receptor (S1R) in milligram quantities were performed. The method of incorporation of the S1R into nanodiscs that mimics the properties of the original biological membrane was learned. Further, learned techniques will be used in studies to find new positive allosteric modulators of S1R as potential memory-enhancing drugs for prevention of disorders of memory processes caused by neurodegenerative disease in LIOS.

Dates of visit: 01.02.2016-30.06.2016.

Status: Implemented.

 

33. Igor Vozny

Host institution: Laboratory of Organic Chemistry, Wageningen University, The Netherlands

Aim: synthesis and preparation of self-assembling compounds

Results: New derivatives for investigations of self-assembling systems were obtained. Experience in work organization, and design, synthesis and preparation of self-assembling compounds was acquired.

Dates of visit: 05.01.2016-01.06.2016.

Status: Implemented.

 

34. Laura Krasnova

Host institution: University of Ljubljana, Slovenia

Aim: Advanced methods in synthesis of nitrogen containing heterocycles

Results: Within this project, several methods of the synthesis of diazenedicarboxamides starting from the appropriate isocyanates and anilines have been learned and diazenedicarboxamide derivatives of pyridine-2(1H)-ones and pyrimidin-2(1H)-ones as potential multidrug resistance modulators have been synthesized. A series of potential multidrug resistance modulators have been obtained and their biological activity will be tested in Latvian Institute of Organic Synthesis.

Dates of visit: 01.02.2016-29.04.2016.

Status: Implemented.

 

35. Egils Bisenieks

Host institution: Rudjer Boskovic Institute, Croatia

Aim: Study of antiradical activity of various 1,4-dihydropyridine derivatives on cell proliferation.

Results: Promising results about the effects of analogues of 1,4-dihydropyridines (1,4-dihydroisonicotinic acids, carbatone and tiocarbatone) on cell viability and proliferation were ontained.

Dates of visit: 17.01.2016-16.04.2016.

Status: Implemented.

 

36. Imanta Brūvere

Host institution: Rudjer Boskovic Institute, Croatia

Aim: Study of antiradical activity of various 1,4-dihydropyridine derivatives in neurodegenerative processes.

Results: The effects of analogues of 1,4-dihydropyridine on cell viability and proliferation were monitored. Several compounds showed enchanced sensivity of cancer cells in regards to normal cells.

Dates of visit: 17.01.2016-17.05.2016.

Status: Implemented.

 

37. Vitālijs Romanovs

Host institution: University of Rennes 1, Rennes, France

Aim: Coordination of synthetic efforts aiming redox active and spin-switching biologically active organogermanium derivatives.

Results: Design and synthesis of a number so far not known classes of organometallic compounds (P®Si and N®Sn hypercoordinated derivatives). Development of a new organic method of interface labelling with electro-commutable paramagnetic nitroxyl probes, and physico-chemical study of the prepared compounds by electrochemistry.

Dates of visit: 06.01.2016-07.04.2016.

Status: Implemented.

 

38 Kārlis Pajuste

Host institution: Institute of Technology, University of Tartu, Estonia

Aim: Preparation of modified 1,4-DHP based delivery systems, Development of delivery systems for DNA transport, studies of physical chemical and biological properties of nanosystems.

Results: In one complex molecule it was successfully combined lipophilic 1,4-DHP derivative and charged protein providing a new type of DNA delivery systems. New kinds of delivery systems for DNA transfection were obtained, however future optimisation is still necessary.

Dates of visit: 03.01.2016-12.03.2016.

Status: Implemented.

 

39. Raivis Žalubovskis

Host institution: University of Florence, Neurofarba Department, Section of Pharmaceutical Chemistry, Italy

http://www2.chim.unifi.it

Aim: Obtaining expertise in molecular mechanisms and biological action of carbonic anhydrases

Results: During the visit modern approaches in construction of anti-infective agents were learned.

Dates of visit: 11.01.2016-25.01.2016

Status: Implemented.

 

40. Oskars Kodoliņš

Host institution: Loughborough University, UK

Aim: Transfer the knowledge in the development of enantioselective organocatalytic reactions

Results: During the experience exchange stay in the group of prof. A. Malkov intramolecular azo-ene reaction was studied. Various methods of inducing enantioselectivity in this reaction were investigated. Experience related to preparation and reactivity of azo-dienes was acquired.

Dates of visit: 01.02.2016-01.07.2016.

Status: Implemented.

 

41. Kristīne Voļska

Host institution: Daniel Swarovski Research Laboratory, Innsbruck Medical University, Austria

Aim: Learn latest methods for determining mitochondrial function that are used for drug discovery

Results: New experimental techniques – mictochondrial membrane potential measurements with fluorimetry or potentiometry with ISE were learned

Dates of visit: 29.02.2016-9.04.2016.

Status: Implemented.

 

42. Elīna Makarova

Host institution: University of Zurich, Switzerland

Aim: Learn advanced methods in biochemistry, molecular and cell biology

Results: New experimental techniques - transient transfections and luciferase reporter assay were learned.

Dates of visit: 29.02.2016-01.04.2016.

Status: Implemented.

 

43. Edijs Vāvers

Host institution: Uppsala University, BMC, Sweden

Aim: Learn new methods for traumatic brain injury studies in mice and rats using fluid percussion and controlled cortical impact models

Results: During the visit fluid percussion and controlled cortical impact models were learned

Dates of visit: 09.02.2016-12.02.2016.

Status: Implemented.

 

44. Līga Zvejniece

Host institution: Uppsala University, BMC, Sweden

Aim: Learn new methods for traumatic brain injury studies in mice and rats using fluid percussion and controlled cortical impact models

Results: During the visit several methods how to induce thaumatic brain injury were learned

Dates of visit: 09.02.2016-12.02.2016.

Status: Implemented.

 

45. Edijs Vāvers

Host institution: University of Eastern Finland, Institute of Clinical Medicine, Kuopio, Finland

Aim: Participation in studies of experimental animal behaviour models for stroke research

Results: Edijs Vavers participated in stroke research and learned methods for animal behavior evaluation after ischemic brain damage in different animal models of stroke. He worked also on the validation of modified sticky-tape and Vermicelli pasta handling tests. During the visit Edijs learned basic principles of histology and immunohistochemistry.

Dates of visit: 15.02.2016-15.04.2016.

Status: Implemented.

 

46. Olesja Koleda

Host institution: University of Rostock, Germany

http://www.uniroma1.it/dottoratoscifarm

Aim: Obtaining expertise in electroorganic synthesis at Dr. R. Francke research group

Results: Electroorganic synthesis of several benzoxazolones or thiobenzalides towards benzothiazoles was performed starting from electrochemically generated reagents.

Dates of visit: 01.03.2016-30.07.2016.

Status: Implemented.

 

47. Dace Rasiņa

Host institution: Perugia University, Italy

http://www.chm.unipg.it/greensoc

Aim: Application of heterogeneous metal catalysis in organic chemistry

Results: Arylation reactions for specific substrates, reaction conditions were studied and optimised. Recycling of heterogenous catalyst was demonstrated.

Dates of visit: 31.08.2014-29.01.2016.

Status: Implemented.

 

48. Guna Sakaine

Host institution: Institution: Antwerp Drug Design Network, University of Antwerp, Belgium.

Aim: Gathering expertise in synthesis of potential phosphodiesterase inhibitors

Results: 16 new potential phosphodiesterase inhibitors for neglected parasitic diseases were synthesized. Some chemical strategy problems with introduction of functional groups were solved. Few synthesized compounds were tested for biological activity.

Dates of visit: 20.03.2016-20.08.2016.

Status: Implemented.

 

49. Edgars Paegle

Host institution: University of Lorraine in Metz (previously - University of Metz), France

http://www.srsmc.univ-lorraine.fr/spip3011/?-Presentation-&lang=fr

Aim: Gathering expertise in synthesis of organoselenium compounds in the research of organoselenium compounds

Results: The work done during the visit mainly was devoted to exploration of electronic effects on the demethylation and/or demethylation/intramolecular cyclization of (6-methoxy-2-(4-methoxyphenyl)benzo[b]thiophen-3-yl)(phenyl)methanone and (6-methoxy-2-(4-methoxyphenyl)benzo[b]selenophen-3-yl)(phenyl)methanone derivatives and their corresponding reduced forms (alcohols instead of ketones). Consequently, new type of polycyclic benzo[b]selenophene derivatives (10H-benzo[b]indeno[2,1-d]selenophene based) was obtained, which is interesting particularly due to the close geometric resemblance with the molecular scaffold of promising selenium analogues of raloxifene.

Dates of visit: 14.03.2016-14.06.2016.

Status: Implemented.

 

50. Mārtiņš Ruciņš

Host institution: Palacký University Olomouc, Czech Republic

http://ach.upol.cz/en/laborator-elektromigracnich-metod.php

Aim: Studies and characterisation of cationic group-containing compounds with analytical methods

Results: Participation in capillary electrophoresis research in three subprojects: electrophoretic desalting experiments for mass spectrometry using ambient ionization techniques. The developed method can be used for pharmacological characterization of drugs in body fluids; Separation of PEG derivatives by micellar electrokinetic chromatography. The method for separation of PEG-derivatives with different long chain without any chromophore was developed using MEKC; Study of discontinuous electrolyte systems in capillary zone electrophoresis. Experimental and theoretical study on changing composition of electrolytes in inlet and outlet vial and capillary was performed.

Dates of visit: 14.03.2016-13.08.2016.

Status: Implemented.

 

51. Iveta Luntēna

Host institution: UniversityLeiden, the Netherlands

http://medchem.leidenuniv.nl

Aim: Synthesis and evaluation of allosteric ligands for G protein-coupled receptors

Results: Learned new methods for synthesis for covalent inhibitors of the adenosine A1 receptor. During the visit putative inhibitors based on thiopyridine and thiopyrimidine core have been synthesised. Optimisation of synthetic road has been also performed.

Dates of visit: 31.03.2016-31.08.2016.

Status: Implemented.

 

52. Maija Dambrova

Host institution: Antwerp Drug Discovery Network, Belgium

Aim: Exchange of experience in research & innovation management and technology transfer.

Results: As a result, it was agreed to collaborate with the Antwerp Drug Discovery Network (ADDN) in the area of testing of novel compounds. Possibilities to participate in HORIZON 2020 forthcoming calls were discussed.

Dates of visit:  14.03.2016-24.03.2016

Status: Implemented.

 

53. Dace Tirzite

Host institution: Antwerp Drug Discovery Network, Belgium

Aim: Exchange of experience in research & innovation management and technology transfer.

Results: As a result, it was agreed to collaborate with the Antwerp Drug Discovery Network (ADDN) in the area of testing of novel compounds. Possibilities to participate in HORIZON 2020 forthcoming calls were discussed.

Dates of visit:  14.03.2016-24.03.2016

Status: Implemented.

 

54. Ruslans Muhamadejevs

Host institution: University of Tartu, Estonia

Aim: Application of Computational Methods in Chemistry

Results: Obtained QSAR model for multiple drug resistance (MDR) modulation activity of thieno[2,3-b]pyridines and furo[2,3-b]pyridines on P-gp, MRP1 and BCRP1 proteins and model for intracellular calcium channel inhibition.

Dates of visit: 8.02.2016-09.07.2016.

Status: Implemented.

 

55. Andrejs Pelšs

Host institution: University of Bristol, UK
Aim: investigation of alternative methodologies of attachment of side chains in prostaglandin synthesis

Results: New synthetic methods of transformation of "Aggarwal enal" intermediate into useful compound  for the obtaining of recently  isolated Δ12-prostaglandin PGJ3 which possesses anticancer activity against leukaemia cells.

Dates of visit: 01.04.2016-30.08.2016.

Status: Implemented.

 

56. Diāna Borovika

Host institution: Institute of Biostructure and Bioimaging of the National Research Council of ltaly, Naples

Aim: Protein expression, purification and crystallization.

Results: During the visit expression, purification and crystallization of different proteins were done. To increase the yield of the proteins, optimization of expression was prepared. To investigate protein-protein interactions, binding assays of obtained proteins were performed.

Dates of visit: 21.03.2016-13.08.2016.

Status: Implemented.

 

57. Anete Parkova

Host institution: University of Oxford, Oxford, UK

Aim: Synthesis of cyclic boronic acid derivatives for use as inhibitors of metallo β-lactamases.

Results: A synthesis of six and five membered boronic acid derivatives has been carried out. A suitable protecting group, a convenient method for synthesis of boronate derivative with pinanediol boronic ester; suitable conditions for Matteson's boronic ester homologation and conditions for boronic ester hydrolysis have been also found.

Dates of visit: 19.04.2016-18.06.2016.

Status: Implemented.

 

58. Bobileva Olga

Host institution: VU Amsterdam (Vrije Universiteit Amsterdam)

Aim: to gain  experience  in fragment-based   drug discovery  as  well  as  in  G-protein  coupled   proteins  (GPCRs)   allosteric  ligands discovery.

Results: The retrosynthetic analysis of non-steroidal FXR agonist GW4064 was performed. Eleven GW4064 fragments and fragment analogues were synthesized for further biological studies.

Dates of visit: 01.04.2016-31.08.2016.

Status: Implemented.

 

59. Aiga Grandāne

Host institution: Leibniz Institute for Catalysis (Rostock, Germany)

http://www.catalysis.de/

Aim: Development of base-free catalytic Wittig reaction.

Results: Optimization of intramolecular base-free catalytic Wittig reaction was done and a series of the target compounds with a potential biological activity were obtained.

Dates of visit: 04.04.2016-26.08.2016

Status: Implemented.

 

60. Olga Konstantinova

Host institution: Aalto University, Helsinki
http://users.tkk.fi/~akoskine
http://chemistry.aalto.fi/en/research/koskinen_group

Aim:  Elaboration of new synthetic approach to the total synthesis of C1-C8 fragment of calyculin C.

Results: We have developed two optional synthesis routes for diene a key intermediate in the synthesis of the hydrophobic tail of calyculin C. We have also described an efficient route for the preparation of iodonitrile derivative in four steps, that can be used in the Suzuki-Miyaura coupling.

Dates of visit: 06.04.2016-08.07.2016.

Status: Implemented.

 

61. Anna Nikitjuka

Host institution: University of Oxford, Oxford, UK

Aim: Evolved P450 mutants as general oxidation catalysts: synthesis via late-stage oxidation. Research area falls under following headings: achieving difficult oxidations and facilitating target synthesis of novel, selective herbecides of viridiol (furanosteroid) group. Retrosynthetic considerations were based on a dual skeleton-building/late stage oxidation strategy.
Results: The total synthesis of viridiol analogue  using the late stage P450-oxidation approach was investigated.  Construction of the furanosteroid core by short skeleton-building sequence, carrying through minimal oxy-functionalities was realized. The research should be continued exploring P450 oxidation at both the activated (benzylic) and unactivated sites of the viridiol analogue.

Dates of visit: 10.04.2016-30.08.2016.

Status: Implemented.

 

62. Arkādijs Soboļevs

Host institution: Cadiz University, Spain

Aim: Gathering expertise in synthesis of natural products

Results: Learned methodologies for a total synthesis of complex natural and non-natural compounds with multiple chiral centers in enantiopure form including multiple chiral centers. The obtained knowledge will be applied at LIOS.

Dates of visit: 12.04.2016-26.04.2016.

Status: Implemented.

 

63. Aiva Plotniece

Host institution: Cadiz University, Spain

Aim:To get access to novel methods and strategies addressing difficult synthetic problems.

Results: During the visit modern catalytic methodologies and optimisation approaches in construction of various molecules were learned. The obtained knowledge will be applied at LIOS.

Dates of visit: 12.04.2016-26.04.2016.

Status: Implemented.

 

64. Maija Kurtenoka

Host institution:  Institute of Biotechnology of Vilnius University, Lithuania

Aim: Synthesis and studies of Carbonic anhydrase inhibitors

Results: Preparation of key intermediates for the synthesis of inhibitors of carbonic anhydrases

Dates of visit: 03.04.2016-30.04.2016.

Status: Implemented.

 

65. Mārtiņš Otikovs

Host institution:   University of Gothenburg, Sweden

Aim: To gain necessary knowledge and skills to setup and optimize nuclear magnetic resonance (NMR) relaxation dispersion experiments to study dynamics of biomacromolecules in milli- to microsecond range.

Results: 15N single quantum relaxation dispersion NMR spectra for wild type protein and mutants of N-terminal domain of E. australis major ampullate spidroin have been acquired. The analysis of acquired spectra has given insight in the dynamics on millisecond timescale for analysed proteins. It was possible to identify exact regions of studied proteins that undergo exchange. The information about structural segments experiencing structural exchange has given insight into dimerization mechanism of N- terminal domain of E. australis major ampullate spidroin.

Dates of visit: 04.05.2016-20.05.2016.

Status: Implemented.

 

66. Baiba Švalbe

Host institution:  Tartu  University, Estonia

Aim: studies of methods for development of genetic modification laboratory animals and specific care practices of it.

Results: The acquired practices used in recombinant animal strain development could be introduced in Institute of Organic Synthesis of Latvia in future research for pharmacological characterization of drugs. Also the acquired knowledge will help to improve welfare of the recombinant animals in future.

Dates of visit: 02.05.2016-04.06.2016.

Status: Implemented.

 

67. Jānis Liepiņš

Host institution: Tartu University, Estonia

Aim: to obtain necessary practical skills in field of yeast gene engineering

Results: All steps necessary for S. cerevisiae genome gene targeting were performed. As a result S. cerevisiae strain with introduced Myc7 C-tag in transcription factor was made. FACS analyses revealed differences in portion of S. cerevisaie cells in G1/G2 cycle phase depending on nutrient source. The acquired knowledge of S. cerevisiae gene editing technique will facilitate it's use for future pharmacological research (like, test system for hight throughput drug screens). 

Dates of visit: 02.05.2016-04.06.2016.

Status: Implemented.

 

68. Raivis Žalubovskis

Host institution: University of Florence, Neurofarba Department, Section of Pharmaceutical Chemistry, Italy

http://www2.chim.unifi.it

Aim: Familiarization with construction of new anti-bacterial agents based on inhibition of bacterial  carbonic  anhydrases  and discussions  of further collaboration  opportunities

Results:  Knowledge on construction of novel type anti-bacterial agents was obtained. The obtained data will be applied at LIOS.

Dates of visit: 13.06.2016-28.06.2016

Status: Implemented.

 

69. Jekaterīna Ivanova

Host institution: University of Jyväskylä, Finland

https://www.jyu.fi/kemia/tutkimus/orgaaninen/en/research/Pihko
https://www.jyu.fi/kemia/tutkimus/orgaaninen/en/research/Pihko/Group%20activities

Aim: participation in research programm of prof. Pihko group on design and synthesis of new organocatalysts

Results: Besides inherent experience on work organization, electron rich iminium catalysts for enantioselective Mukaiyama-Michael reaction were synthesized during the visit. The synthesis of known pyrrolidine-derived catalyst was successfully scaled up to multigram scale. A route to a new indole-based catalyst was developed and the catalyst was evaluated for its reactivity and enantioselectivity in Mukaiyama-Michael reaction. The results of this work will be presented at international conferences and symposiums. The outgoing visit will promote future collaboration between LIOS and Wageningen University.

Dates of visit: 15.06.2016-30.08.2016

Status: Implemented.

 

70. Aleksandrs Pustenko

Host institution: University of Jyväskylä, Finland

https://www.jyu.fi/kemia/tutkimus/orgaaninen/en/research/Pihko
https://www.jyu.fi/kemia/tutkimus/orgaaninen/en/research/Pihko/Group%20activities

Aim: to scale up synthesis of previously designed and synthesised pyrrolidine catalyst in prof. Pihko group, design and synthesis of new indole-based pyrrolidine catalyst.

Results: Besides inherent experience on work organization, a successful scale up for a pyrrolidine catalyst that has been designed and synthesised in prof. Pihko group earlier was done, also development and synthesis of new electron poor pyrrolidine catalyst with indole-based design. Indole-based pyrrolidine catalyst has been tested in enantioselective Mukaiyama-Michael reaction. The synthesis was based on known methods although some improvements and changes in these methods were made.

As soon as desired pyrrolidine catalyst with indole function was obtained, it was tested in enantioselective Mukaiyama-Michael reaction. Unfortunately no enantioselectivity improvements were made, that means catalyst should be optimized.

Dates of visit: 15.06.2016-30.08.2016

Status: Implemented.

 

71. Marina Makrecka-Kūka

Host institution: Innsbruck Medical University, Austria

http://www.bioblast.at/index.php/Gnaiger_E

Aim: learning of novel advanced  approaches  for studying  mitochondrial  function  in physiology  and pathology

Results: The novel advanced approaches  to study mitochondrial  function  in physiology  and pathology were learned and will  be used in Latvian  Institute of Organic Synthesis for pharmacological  characterization  of mitochondrial  targeted compounds.

Dates of visit: 07.07.2016-13.07.2016.

Status: Implemented.

 

72. Jānis Kūka

Host institution: Innsbruck Medical University, Austria

http://www.bioblast.at/index.php/Gnaiger_E

Aim: Introduction to advanced methods for studying  of mitochondrial  function 

Results: The novel methods of different  mitochondrial  preparations  were learned and will  be used in Latvian  Institute of Organic Synthesis for screening and pharmacological characterization  of mitochondrial  targeted drugs.

Dates of visit: 07.07.2016-13.07.2016.

Status: Implemented.

 

73. Maija Kurtenoka

Host institution:   Institute of Biotechnology of Vilnius University, Lithuania

Aim: Participation in studies of carbonic anhydrases as anticancer drug targets carried out by Dr. Matulis research group

Results: Preparative synthesis of a series of novel CAIX inhibitors, based on fluorinated benzenesulfonamides  scaffold

Dates of visit: 31.05.2016-30.07.2016.

Status: Implemented.

 

74. Inguna Goba

Host institution: Helmholtz Zentrum München (Technische Universität München), Germany

Aim: Membrane protein incorporation into nanodiscs, NMR studies of membrane protein-ligand complexes.

Results: 15N, 2D labelled Sigma-1 receptor construct (S1RFL (223aa) and S1R-H1del (34-223aa)) fused to GFP was expressed in E.coli cells and purified in detergent (n-Dodecyl β-D-maltoside, DDM) to homogeneity. Purification of the S1R was performed using a combination of immobilized metal ion affinity chromatography (IMAC) and gel filtration. Incorporation of S1R into MSP1D1 nanodiscs resulted in protein oligomerization. 2D NMR spectra of S1R in detergent were recorded.

Dates of visit: 07.07.2016-30.08.2016.

Status: Implemented.

 

75. Raivis Žalubovskis

Host institution: jaud University of Florence, Neurofarba Department, Section of Pharmaceutical Chemistry, Italy

http://www2.chim.unifi.it

Aim: Participation in research carried out at University of Florence (C.T. Supuran group) on the field of construction of anti-infective agents.

Results: Knowledge and experience on the construction of new inhibitors of carbonic anhydrases as potential anti-infective agents were obtained.

Dates of visit: 12.07.2016-16.08.2016

Status: Implemented.

 
Updated 31.08.2016