Recent publications

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.

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.

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.

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.

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.

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.

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.

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

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

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), 2014, 10, 1583—1589, DOI 10.1007/s10593-014-1610-4.

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.

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.

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: 10.1021/ml4004952.

Nikitjuka, A.; Jirgensons, A. Synthesis, Chemical and Biological Properties of Aziridine-1-carbaldehyde oximes (review). Chemistry of Heterocyclic Compounds (russ) 2013, 11, 1669-1684, DOI: 10.1007/s10593-014-1407-5. Dedicated to Professor Jānis Stradiņš on the occasion of his 80 anniversary.

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.

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.

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

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

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. Chem. Heterocycl. Compd. (russ), 2012, N6 (540), 989-994. Dedicated to professor Ivars Kalvinsh on the occasion of his 65th birthday.

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.

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

Grigorjeva, L.; Jirgensons, A. 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.

Maleckis, A.; Klimovica, K.; Jirgensons, A. 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.

Usachova, N.; Leitis, G.; Jirgensons, A.; Kalvinsh I. 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.

Recent patents

Wikberg, J.; Jirgensons A., Liepinsh E. Novel Compounds, Their Manufacture and Uses (II). Patent No WO2013110744, A2, 01.08. 2013.

Gold M. R.; Kauss V.; Jirgensons A; Method For Preparing Neramexane or a Salt Thereof. Patent No WO2011035924, A1, 31. 03. 2011.

Gold, M. R.; Jirgensons, A; Huber, F. A. M. Method For Producing Memantine. WO 2010/069555 A1, 24. 06. 2010.

Maleckis, A.; Jirgensons, A. Enantioselektīva 2-trihlormetil-4-viniloksazolīna iegūšana, P-09-77. 2009

Finn, P; Robinson, D.; Kham, N.; Jirgensons, A.; Leitis, G.; Kalvinsh I. Bicyclosulfonyl acid (BCSA) Compounds and Their Use as Therapheutic Agents PCT /GB2008/001683, 16.05.2008

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.

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