Aigars Jirgensons

Curriculum Vitae

Personal details

Name: Aigars Jirgensons

Date of birth: September 14, 1973

Nationality: Latvian

Education

2002 (jan-dec) Post-doctoral studies, University of Perugia, Italy. Group of professor R. Pellicciari.

2000 Dr. Chem., Chemistry Department at University of Latvia.

1997 M.Sc. Chem., Chemistry Department University of Latvia.

1995 B.Sc. Chem., Chemistry Department at University of Latvia.

Carrier details

Latvian Institute of Organic Synthesis

2006 Head of the group at Latvian Institute of Organic Synthesis.

2004 Senior researcher at Latvian Institute of Organic Synthesis.

2001 Researcher at Latvian Institute of Organic Synthesis.

1991 Assistant at Latvian Institute of Organic Synthesis

Riga Technical University

2011 Associate professor

2007 Docent

List of publications

42. Rasina, D.;  Otikovs, M.; Leitans, J; . Recacha, R.; Borysov, O. V.;  Kanepe-Lapsa, I.; Domraceva, I.; Pantelejevs, T.;  Tars, K.;  Blackman, M. J.; Jaudzems, K.;  Jirgensons,  A. Fragment-Based Discovery of 2-Aminoquinazolin-4(3H)-ones As Novel Class Nonpeptidomimetic Inhibitors of the Plasmepsins I, II, and IV. J. Med. Chem. 2015, article asap, DOI; 10.1021/acs.jmedchem.5b01558.

41. Recacha R.; Leitans J.; Akopjana I.; Aprupe L.; Trapencieris P.; Jaudzems K.; Jirgensons A.; Tars K. Structures of plasmepsin II from Plasmodium falciparum in complex with two hydroxyethylamine-based inhibitors. Acta Cryst. 2015. F71, 1531-1539, DOI:10.1107/S2053230X15022049.

40. Sirotkina, J.; Grigorjeva, L.; Jirgenons, A. Synthesis of Alkynyl Glycinols via Lewis Acid Catalyzed Propargylic Substitution of bis-Imidates. Eur. J. Org. Chem., 2015. 31, 6900-6908, DOI: 10.1002/ejoc.201500937.

39. Nikitjuka, A.; Shestakova, I.; Romanchikova, N.; Jirgensons A. Synthesis and biological evaluation of aziridin-1-yl oxime-based vorinostat analogs as anticancer agents. Chem. Heterocycl. Compd., 2015, 51(7), 647-657, DOI 10.1007/s10593-015-1752-z.

38. Skvorcova, M.; Grigorjeva, L; Jirgensons, A. Tetrahydro-1,3-oxazepines via Intramolecular Amination of   Cyclopropylmethyl Cation. Org.Lett., 2015, 17, 2902–2904, DOI: 10.1021/acs.orglett.5b01014.

37. Kumar, V.; Klimovica, K.;  Rasina, D. Jirgensons A. 2-Vinyl Threoninol Derivatives via Acid-Catalyzed Allylic Substitution of Bisimidates. J. Org. Chem., 2015, 80, 5934–5943, DOI: 10.1021/acs.joc.5b00529.

36. Grigorjeva,  L;  Kinens, A.;  Jirgensons,  A. Unsaturated syn- and anti-1,2-Amino Alcohols by Cyclization of Allylic Bis-trichloroacetimidates. Stereoselectivity Dependence on Substrate Configuration. J. Org. Chem., 2015, 80, 920–927, DOI: 10.1021/jo502404y.

35. Nikitjuka, A.;  Nekrasova, A.; Jirgensons, A. Methylprenyl and Prenyl Protection for Sulfonamides. Synlett, 2015, 26, 183-186, DOI: 10.1055/s-0034-1379428.

34. Kher, S. S.; Jirgensons, A. Synthesis of β-amino-α -ketoamides (Review). Curr. Org. Chem., 2014, 18, 2240-2269, DOI: 10.2174/1385272819666140818223225.

33. Kher, S. S.; Penzo, M.; Fulle, S.; Ebejer,  J. P.;  Finn, P. W. ; Blackman, M. J.; Jirgensons, A.  Quinoxaline based inhibitors of malarial protease PfSUB. Chem. Heterocycl. Compd. (russ) 2104, 10, 1583—1589.

32. Kher, S. S.; Penzo, M.; Fulle, S.; Finn, P. W. ; Blackman, M. J.; Jirgensons, A. Substrate derived peptidic α-ketoamides as inhibitors of the malarial protease PfSUB1. Bioorg. Med. Chem. Lett., 2014, 24(18), 4486-4489, DOI: 10.1016/j.bmcl.2014.07.086.

31. Grigorjeva, L.; Liepinsh, E.; Razafimahefa, S.; Yahorau, A.; Yahorava, S.; Rasoanaivo, P.; Jirgensons, A.; Wikberg, J. E. S. Semisynthesis of libiguin A and its analogues by trans-lactonization of phragmalin. J. Org. Chem., 2014, 79 (9), 4148–4153, DOI: 10.1021/jo500318w.

30. Jaudzems, K.; Tars, K.; Maurops, G.; Ivdra, N; Otikovs, M. ; Leitans, J.; Kanepe-Lapsa, I.; Domraceva, I.; Mutule, I.; Trapencieris, P.; Blackman, M. J.; Jirgensons, A. Plasmepsin Inhibitory Activity and Structure-Guided Optimization of a Potent Hydroxyethylamine-Based Antimalarial Hit. ACS Med. Chem. Lett., 2014, 5(4), 373–377, DOI: org/10.1021/ml4004952

29. Katkevica, S.; Salun, P.; Jirgensons, A. Synthesis of 5-Substituted 3-Mercapto-1,2,4-Triazoles via Suzuki–Miyaura reaction. Tetrahedron Lett., 2013, 54, 4524–4525, DOI: 10.1016/j.tetlet.2013.06.067.

28. Jirgensons, A.; Grigorjeva, L.; Maleckis, A.; Klimovica, K. Unsaturated Amino Alcohols via Cyclization of Allylic Bistrichloroacetimidates. Synlett, 2013, 24(18) 2345-2349,  DOI: 10.1055/s-0033-1338977.

27. Nikitjuka, A.; Jirgensons, A. Synthesis, Chemical and Biological Properties of Aziridine-1-carbaldehyde oximes (review). Chem. of Heterocycl. Comp. (russ) 2013, 11, 1669-1684. Dedicated to Professor Jānis Stradiņš on the occasion of his 80 anniversary

26. Withers-Martinez, C.; Suarez, C.; Fulle, S.; Kher, S.; Penzo, M.; Ebejer, J.-P.; Koussis, K.; Hackett, F.; Jirgensons, A.; Finn, P.; Blackman, M. J. Plasmodium subtilisin-like protease 1 (SUB1): Insights into the active-site structure, specificity and function of a pan-malaria drug target. International Journal for Parasitology 2012, 42, 597-612, DOI: 10.1016/j.ijpara.2012.04.005.

25. Grigorjeva, L; Maleckis, A; Klimovica, K.; Skvorcova, M; Ivdra, N.; Leitis, G.; Jirgensons, A. Novel synthesis of 2-trichloromethyl-4-vinyl-oxazoline and its derivatization by ring cleavage reactions. Chemistry of Heterocyclic Compounds (russ) 2012, N6 (540), 989-994. Dedicated to professor Ivars Kalvinsh on the occasion of his 65th birthday.

24. Grigorjeva, L.; Jirgensons, A. Synthesis of Cyclic N-Tosyl-iminocarbonates by Lewis Acid Catalysed Allylic Substitution of Trichloroacetimidates. Eur. J. Org. Chem.,27,5307–5316, 2012, DOI: 10.1002/ejoc.201200378.

23. Nikitjuka, A; Jirgensons, A. Synthesis of Hydroxamic Acids by Using the Acid Labile O-2-Methylprenyl Protecting Group. Synlett 2012,23(20), 2972-2974, DOI: 10.1055/s-0032-1317687.

22. L. Grigorjeva, A. Jirgensons Lewis Acid Catalyzed Intramolecular Allylic Substitution of Bis(trichloroacetimidates): A Versatile Approach to Racemic Unsaturated Amino Acids. Eur. J. Org. Chem., 2011, 2421–2425, DOI: 10.1002/ejoc.201100060.

21. K. Klimovica, L. Grigorjeva, A. Maleckis, J. Popelis, A. Jirgensons C-Quaternary vinylglycinols by metal catalysed cyclization of allylic bis-trichloroacetimidates. Synlett, 2011, 2849-2851,DOI:10.1055/s-0031-1289537.

20. N. Usachova, G. Leitis, A. Jirgensons, I. Kalvinsh Synthesis of hydroxamic acids by activation of carboxylic acids with N,N’-carbonyldiimidazole: exploring the efficiency of the method. Synthetic Comm., 2010, 40, 927–935,DOI: 10.1080/00397910903026723.

19. A. Maleckis, K. Klimovica A. Jirgensons Catalytic Enantioselective Synthesis of 4-Vinyl-2-Trichloromethyloxazoline: an Access to Enantioenriched Vinylglycinol surrogate. J. Org. Chem., 2010, 75, 7897-7900, DOI: 10.1021/jo101781y.

18. M. Teus, A. Jirgensons, M. Dambrova, R. Mezhapuke, C. G. Parsonsand W. Danysz. Identification of GCP II Inhibitors Based on 4-Arylmethyl-3-(4-carboxyphenyl)-5-hydroxyisoxazole Scaffold. Letters in Drug Design & Discovery, 2009, 6, 29-32.

17. А. Grigorjeva, А. Jirgensons, I. Domracheva, E. Jaschenko, I. Shestakova, V. Andrianov, I. Kalvinsh Synthesis of novel (1-aziridinyl-1-hydroxyiminomethyl)arenes and their citotoxic activity Chemistry of Heterocyclic Compounds 2009, 45, 203-213.

16. A. Maleckis, I. Jaunzeme, A. Jirgensons Cyclization of Trichloroacetimidates via Olefin Aminopalladation b-Heteroatom Elimination Route Eur. J. Org. Chem., 2009, 6407–6412.

15. I. Jaunzeme, A Jirgensons. Ether-directed diastereoselectivity in catalysed Overman rearrangement: Comparative studies of metal catalysts. Tetrahedron 2008, 64, 5794-5799

14. T. Noeske, A. Jirgensons, I. Starchenkovs, S. Renner, I. Jaunzeme, D. Trifanova, M. Hechenberger, T. Bauer, V. Kauss, C. G. Parsons, G. Schneider, T. Weil Virtual Screening for Selective Allosteric mGluR1 Antagonists and Structure-Activity Relationship Investigations for Coumarine Derivatives. ChemMedChem 2007, 2, 1763-1773.

13. K. Gilling, C. Jatzke C. Wollenburg, M. Vanejevs, V. Kauss, A Jirgensons, C. G. Parsons A novel class of amino-alkylcyclohexanes as uncompetitive, fast, voltage- dependent, N-methyl-D-aspartate (NMDA) receptor antagonists – in vitro characterization. Journal of Neural Transmission 2007, 114, 1529-1537.

12. М. Теус, А. Иргенсонс, М. Дамброва, Р. Межапуке. Синтез и ГКП II ингибиторная активность гетероциклических аналогов 4-[4-(3-бромбензил)-5-гидроксиизоксазол-3-ил]бензойной кислоты. HГC 2007, 1693-1697.

11. J. Nagel, I.Belozertseva, S. Greco, V. Kashkin, A. Malyshkin, A. Jirgensons, E. Shekunova, B. Eilbacher, A. Bespalov and W. DanyszEffects of NAAG peptidase inhibitor 2-PMPA in model chronic pain – relation to brain concentration. Neuropharmacology 2006, 51, 1163-1173.

10. M. Teus, A. Jirgensons, M. Dambrova, C. Parsons Dikarbonskābju iegūšana 3-fenil-5-hidroksiizoksazolu rindā un to glutamāta karboksipeptidāzes II inhibitorā aktivitāte. RTU Zinātniskie raksti 2006, 12, 7-14.

9. I. Jaunzeme, A. Jirgensons, V. Kauss, E. Liepins Diastereoselectivity in the Overman rearrangement of O-cyclohexylideneethylimidates. Tetrahedron Lett. 2006, 3885-3887.

8. I. Jaunzeme, A. Jirgensons Novel Catalysts for Overman Rearrangement. Synlett 2005, 2984-2986.

7. A. Jirgensons. M. Marinozzi, R. Pellicciari Conformationally constrained amino acids: enetiodivergent synthesis of all four diastereomers of 2-(tetrahydrofuran-2-yl)glycine. Tetrahedron 2005, 61, 373-377.

6. D. Trifanova, M. Trifonova, A. Jirgensons, V. Kauss, O. Pugovich, I. Kalvinsh, G. Quack The synthesis of potential Neramexane metabolites: cis- and trans-3-amino-1,3,5,5-tetramethylcyclohexanecarboxylic acids. Tetrahedron Lett. 2004, 45, 8145-8147.

5. W. Danysz., C.G. Parsons, A. Jirgensons., V. Kauss, J. Tillner Amino-alkyl-cyclohexanes as novel pharma ceuticals of uncompetitive NMDA receptor antagonists. Curr. Pharm. Design, 2002, 8, 434-437.

4. A. Jirgensons, V. Kauss, I. Kalvinsh, M. R. Gold, A practical synthesis of tert-carbinamines via the Ritter reaction with chloroacetonitrile. Synthesis, 2000, 1709-1712.

3. A. Jirgensons, V. Kauss, I. Kalvinsh, M. R. Gold, W. Danysz, C. G. Parsons, G. Quack, Synthesis and structure – affinity relationships of 1,3,5-alkylsubstituted cyclohexylamines binding at NMDA receptor PCP site. Eur. J. Med. Chem., 2000, 35, 555-565.

2. A. Jirgensons, V. Kauss, A. F. Mishnev, I. Kalvinsh, The synthesis of 3-amino-3-methylbicyclo[3.3.1] nonanes. Endo-selectivity in the Ritter reaction of 1,3,5,7a-tetramethylbicyclo[3.3.1]nonan-3-ol. J. Chem. Soc., PT 1, 1999, 3527-3530.

1. A. Jirgensons, I. Kums, V. Kauss, I. Kalvinsh, A Convenient reagent for N-hydroxyguanylation. Synth. Comm., 1997, 27, 315-322.

Patents

  1. M. Gold, W. Danysz, C. G. Parsons, I. Kalvinsh, V. Kaussand A. Jirgensons Novel uncompetitive antagonists of the NMDA receptor: amino-cyclohexane derivatives Appl. No 09/141/,381, 27.09.1998, Patent No 6,034,134, 07.03.2000.
  2. M. Gold, W. Danysz, C. G. Parsons, I. Kalvinsh, V. Kaussand A. Jirgensons Novel uncompetitive antagonists of the NMDA receptor: amino-cyclohexane derivatives Appl. No 09/141/,380, 27.09.1998, Patent No 6,071,966, 06.06.2000.
  3. J. M. Kelly, I. Kalvinsh, V. Kauss, A. Jirgensons, M. Gold. 1-Amino-alkylcyclohexane derivatives as trypanocidal agents 2002, WO 2/24186 A1.
  4. M. Henrich, W.Danysz, Ch.G. R. Parsons, I.Kalvinsh, V.Kauss, A.Jirgensons, M.Gold. Unsaturated 1-amino-alkylcyclo-hexane NMDA, 5HT3 and neuronal nicotinic receptor antagonists 2003, Pat US 2003/0166634 A1.
  5. A. Jirgensons, Ch.G. R. Parsons; I. Jaunzeme; I. Kalvinsh; H. Markus; M. Vanejevs; T. Weil; V. Kauss; W. Danysz. Tetrahydroquinolinones and their use as antagonists of metabotropic glutamate receptors. Appl. No US 2005-211829, Patent No US 2006/004001 A1, 2006
  6. Ch.G. R. Parsons; A. Jirgensons; D. Trifanova ; I. Kalvinsh, I. Starchenkovs; M. Henrich; T. Noeske; T. Weil; V. Kauss; W. Danysz. Chromenones and Their Use as Modulators of Metabotropic Glutamate Receptors. Appl. No WO 2006GB03888, 19.10.2006, Patent No WO 2007045876, 26. 04. 2007.
  7. Ch.G. R. Parsons; I. Kalvinsh; D. Trifanova; A. Jirgensons; V. Kauss; T. Weil; W. Danysz; M. Henrich; Adamantyl-(cyclopropyl)-ketones as Metabotropic Glutamate Receptor Modulators. Appl. No WO2007GB03518, 17.09.2007, Patent No WO WO2008035049, 27. 03. 2008.

  8. P. Finn, D. Robinson, N. Kham, A. Jirgensons, G. Leitis, I. Kalvinsh Bicyclosulfonyl acid (BCSA) Compounds and Their Use as Therapheutic Agents Appl. No PCT /GB2008/001683, 16.05.2008

  9. E. Abele; R Abele; V. Bridane; I. Domracheva; L. Golomba; A. Grigorjeva; E. Jaschenko; A. Jirgensons; I. Kalvinsh; I. Shestakova, Cytostatic 1-acylaziridine oximes, Latvijas Republikas Patentu valde, Pieteik. P-08-123, Pieteik. dat. 30.06.2008.
  10. E. Abele; R Abele; V. Bridane; I. Domracheva; L. Golomba; A. Grigorjeva; E. Jaschenko; A. Jirgensons; I. Kalvinsh; I. Shestakova Cytostatic 1-aroylaziridine oximes, Latvijas Republikas Patentu valde, Pieteik. P-08-125, Pieteik. dat. 30.06.2008.
  11. E. Abele; R Abele; V. Bridane; I. Domracheva; L. Golomba; A. Grigorjeva; E. Jaschenko; A. Jirgensons; I. Kalvinsh; I. Shestakova Novel nitrofurylvinylquinolines, Latvijas Republikas Patentu valde, Pieteik. P-08-124, Pieteik. dat. 30.06.2008.
  12. E. Abele; R Abele; V. Bridane; I. Domracheva; L. Golomba; A. Grigorjeva; E. Jaschenko; A. Jirgensons; I. Kalvinsh; I. Shestakova. Cytostatic substituted 1-acylaziridine oximes, Latvijas Republikas Patentu valde, Pieteik. P-08-126, Pieteik. dat. 30.06.2008.
  13. Maļeckis A., Jirgensons A. Enantioselektīva 2-trihlormetil-4-viniloksazolīna iegūšana, Pieteikuma Nr. P-09-77. 2009,
  14. Jirgensons A.; Leitis G.; Kalvinsh I.; Robinson D.; Finn P.; Khan N. Bicyclosulfonyl acid (BCSA) compounds and their use as therapeutic agents WO 2008142376 (A1), 27.11, 2008.
  15. Parsons Ch.G.R.; Jirgensons A.; Jaunzeme I.; Kalvinsh I.; Henrich M.; Vanejevs M.; Weil T.; Kauss V.; Dansyz W. Tetrahydroquinolinones and their use as antagonists of metabotropic glutamate receptors. DK 1723116 (T3), 2.2, 2009.
  16. Gold M. R.; Jirgensons A; Huber F. A. M. Method For Producing Memantine. Patent No WO 2010/069555 A1, 24. 06. 2010.
  17. 17. Gold M. R.; Kauss V.; Jirgensons A; Method For Preparing Neramexane or a Salt Thereof. Patent No WO2011035924, A1, 31. 03. 2011.
  18. Wikberg, J.; Jirgensons A., Liepinsh E. Novel Compounds, Their Manufacture and Uses (II). Patent No WO2013110744, A2, 01.08. 2013.

Comments are closed.