December 23, 2018

Prof. Dr. Aigars Jirgensons

Head of Group, Deputy Director of LIOS for Science

E-mail: aigars@osi.lv

LinkedIn

Curriculum Vitae

Carrier Latvian Institute of Organic Synthesis, Riga, Latvia
Since 2017 Deputy Director of the LIOS for Science
Since 2006 Head of Group
Since 2004 Principal Researcher
2001 Researcher
1991 Research Assistant

Riga Technical University, Riga, Latvia
Since 2016 Full Professor
2011 Associate Professor 
2007 Docent

University of Perugia, Perugia, Italy
2002 (Jan-Dec) Postdoctoral Researcher
Education 2002 (Jan-Dec) Postdoc, University of Perugia (Prof. R. Pellicciari Group)
2000 Dr. Chem., Faculty of Chemistry, University of Latvia
1997 M.Sc. Chem., Faculty of Chemistry, University of Latvia
1995 B.Sc. Chem., Faculty of Chemistry, University of Latvia
AwardsFull Member at Latvian Academy of Science
Member of Experts at Latvian Science Council
Member of Advisory Board at Latvian Science Council
Latvian Representative of EU-OPENSCREEN.
Latvian Representative of EuChemS Organic Chemistry Section
Field Editor of The Journal “ Amino Acids”
2023 Commander of the Order of the Three Stars
2019 Paul Walden’s medal
2018 G. Vanags Prize in Chemistry from Latvian Academy of Science
2017 Full Member of the Latvian Academy of Science
2016 Scientific Achievement of the Year from Latvian Academy of Science
2001 Merz Pharmaceuticals Postdoctoral Fellowship

List of Publications

93. Substrate Analogues Entering the Lipoic Acid Salvage Pathway via Lipoate-Protein Ligase 2 Interfere with Staphylococcus aureus Virulence

Scattolini, A.; Grammatoglou, .; Nikitjuka, A.; Jirgensons, A.; Mansilla, M. C.; Windshügel, B. ACS Infect. Dis. 2024, asap. DOI:10.1021/acsinfecdis.4c00148

92. Design, quality and validation of the EU-OPENSCREEN fragment library poised to a high-throughput screening collection

Jalencas, X.; Berg, H.; Espeland, L. O.; Sreeramulu, S.; Kinnen, F.; Richter, C.; Georgiou, C.; Yadrykhinsky, V.; Specker, E.; Jaudzems, K.; Miletić, T.; Harmel, R.; Gribbon, P.; Schwalbe, H.; Brenk, R.; Jirgensons, A.; Zaliani, A.; Mestres, J. RSC Med. Chem., 2024, 15, 1176-1188. DOI:10.1039/D3MD00724C

91. Structure-based identification of salicylic acid derivatives as malarial threonyl tRNA-synthetase inhibitors

Bobrovs, R.; Bolsakova, J.; Buitrago, J. A. R.; Varaceva, L.; Skvorcova, M.; Kanepe, I.; Rudnickiha, A.; Parisini, E.; Jirgensons, A. PLoS ONE, 2024, 19, e0296995. DOI:10.1371/journal.pone.0296995

90. Spiropyran-Based Photoisomerizable α-Amino Acid for Membrane-Active Peptide Modification

Hrebonkin, A.; Afonin, S.; Nikijuka, A.; Borysov, O. V.; Leitis, G.; Babii, O.; Koniev, S.; Lorig, T.; Grage, S. L.; Nick, P.; Ulrich, A. S.; Jirgensons, A; Komarov, I. V. Chem. – Eur. J., 2024, 30, e202400066. DOI:10.1002/chem.202400066

89. Electrochemical Formation of Oxazolines by 1,3-Oxyfluorination of Non-activated Cyclopropanes

Darzina, M.; Jirgensons, A. Org. Lett., 2024, 26, 2158–2162. DOI:10.1021/acs.orglett.4c00143

88. Discovery of Malarial Threonyl tRNA Synthetase Inhibitors by Screening of a Focused Fragment Library

Bolsakova, J.; Bobrovs, R.; Varacheva, L.; Rudnickiha, A.; Kanepe, I.; Parisini, E.; Jirgensons, A. ACS Med. Chem. Lett. 2024, 15, 76–80. DOI:10.1021/acsmedchemlett.3c00403

87. Exploring the Binding Pathway of Novel Nonpeptidomimetic Plasmepsin V Inhibitors

Bobrovs, R.; Drunka, L.; Kanepe, I.; Jirgensons, A.; Caflish, A.; Salvalaglio, M.; Jaudzems, K. J. Chem. Inf. Model. 2023, 63, 21, 6890–6899. DOI:10.1021/acs.jcim.3c00826

86. Effect of novel furan-based ester reactive diluent on structure and properties of UV-crosslinked acrylated rapeseed oil

Briede, S.; Platnieks, O.; Darzina, M.; Jirgensons, A.; Gaidukovs, S. J. Polym. Sci., 2023, 1. DOI:10.1002/pol.20230451

85. Semisynthesis of Linariophyllenes A–C and Rumphellolide H, Structure Revisions and Proposed Biosynthesis Pathways

Stakanovs, G.; Blazevica, A.; Belyakov, S.; Rasina, D.; Jirgensons, A. J. Nat. Prod., 2023, 86, 2368–2378. DOI:10.1021/acs.jnatprod.3c00574

84. Macrocyclic Peptidomimetic Plasmepsin X Inhibitors with Potent In Vitro and In Vivo Antimalarial Activity

Kovada, V.; Withers-Martinez, C.; Bobrovs, R.; Ce̅rule, H.; Liepins, E.; Grinberga, S.; Hackett, F.; Collins, C. R.; Kreicberga, A.; Jiménez-Díaz, M. B.; Angulo-Barturen, I.; Rasina, D.; Suna, E.; Jaudzems, K.; Blackman, M. J.; Jirgensons, A. J. Med. Chem. 2023, 66, 15, 10658–10680. DOI:10.1021/acs.jmedchem.3c00812

83. Assembling the Methanoindene Cage of Phragmalin-Type Natural Products

Becica, J.; Rāciņš, O.; Ivanova, M.; Jirgensons, A. J. Org. Chem., 2023 88, 10306–10309. DOI:10.1021/acs.joc.3c00952

82. Synthesis and evaluation of an agrocin 84 toxic moiety (TM84) analogue as a malarial threonyl tRNA synthetase inhibitor

Rodriguez Buitrago, J. A.; Leitis, G.; Kaņepe-Lapsa, I.; , A.;  Parisini, E.; Jirgensons, A. Org. Biomol. Chem., 2023,  21, 5433-5439. DOI:10.1039/D3OB00670K

81. 3-(Adenosylthio)benzoic Acid Derivatives as SARS-CoV-2 Nsp14 Methyltransferase Inhibitorswman

Bobileva, O.; Bobrovs, R.; Sirma, E. E.; Kanepe, I.; Bula, A. L.; Patetko, L.; Ramata-Stunda, A.; Grinberga, S.; Jirgensons, A.; Jaudzems, K. Molecules, 2023, 28(2), 768. DOI:10.3390/molecules28020768

80. Synthesis and SAR of phenylazoles, active against Staphylococcus aureus Newman

Solomin, V. V.; Ciruelos, B. F.; Velikova, N.; Wells, J.; Albanese, M.; Adhav, A.; Jirgensons, A. Chem. Heterocycl. Compd., 2022, 58, 737-748. DOI:10.1007/s10593-023-03151-9

79. Intramolecular Friedel–Crafts alkylation by electrochemical carbenium ion generation

Lielpētere, A.; Šilaks, A.; Jirgensons, A. Chem. Heterocycl. Compd., 2022, 58, 732-736. DOI:10.1007/s10593-023-03150-w

78. Subtilisin-like Serine Protease 1 (SUB1) as an Emerging Antimalarial Drug Target: Current Achievements in Inhibitor Discovery

Lidumniece, E.; Withers-Martinez, C.; Hackett, F.; Blackman, M. J.; Jirgensons, A. J. Med. Chem., 2022, 65, 12535-12545. DOI:10.1021/acs.jmedchem.2c01093

77. Functionalization of Tetrazoles Bearing the Electrochemically Cleavable 1N-(6-Methylpyridyl-2-methyl) Protecting Group

Grammatoglou, K.; Dārziņa, M.; Jirgensons, A. ACS Omega, 2022, 7, 18103–18109. DOI:10.1021/acsomega.2c01633

76. Convergent biomimetic semisynthesis of disesquiterpenoid rumphellolide J

Stakanovs, G.; Belyakov, S.; Jirgensons, A.; Rasina, D. Org. Biomol. Chem., 2022, 20, 2455-246. DOI:10.1039/D2OB00238H

75. Exploring Aspartic Protease Inhibitor Binding to Design Selective Antimalarials

Bobrovs, R.; Basens, E. E.; Drunka, L.; Kanepe, I.; Matisone, S.; Velins, K. K.; Andrianov, V.; Leitis, G.; Zelencova-Gopejenko, D.; Rasina, D.; Jirgensons, A.; Jaudzems, K. J. Chem. Inf. Model., 2022, 62, 3263–3273. DOI:10.1021/acs.jcim.2c00422

74. Functionalization of 1N-Protected Tetrazoles by Deprotonation with the Turbo Grignard Reagent

Grammatoglou, K.; Jirgensons, A. J. Org. Chem., 2022, 87, 3810-3816. DOI:10.1021/acs.joc.1c02926

73. Discovery of sars-cov-2 nsp14 and nsp16 methyltransferase inhibitors by high-throughput virtual screening

Babrovs, R.; Kanepe, I.; Narvaiss, N.; Patetko, L.; Kalnins, G.; Sisovs, M.; Bula, A. L.; Grinberga, S.; Boroduskis, M.; Ramata-Stunda, A.; Rostoks, N.; Jirgensons, A. Pharmaceuticals, 2021, 14, 1243. DOI:10.3390/ph14121243

Pharmaceuticals 14 01243 g003 550

72. Torii-Type Electrosynthesis of α,β-Unsaturated Esters from Furfurylated Ethylene Glycols and Amino Alcohols

Darzina, M.; Lielpetere, A.; Jirgensons, A. Eur. J. Org. Chem., 2021, 2021, 4224. DOI:10.1002/ejoc.202100605



71. Synthesis of Indazoles From 2-Formylphenylboronic Acids

Solomin, V. V.; Seins, A.; Jirgensons, A. RSC Adv. 2021, 11, 22710-22714. DOI:10.1039/D1RA04056A



70. Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate

Bobiļeva, O.; Bobrovs, R.; Kaņepe, I.; Patetko, L.; Kalniņš, G.; Šišovs, M.; Bula, A. L.; Grīnberga, S.; Borodušķis, M.; Ramata-Stunda, A.; Rostoks, N.; Jirgensons, A.; Tārs, K.; Jaudzems, K. ACS Med. Chem. Lett. 2021, 12, 1102-1107. DOI:10.1021/acsmedchemlett.1c00140



69. Peptidic boronic acids are potent cell-permeable inhibitors of the malaria parasite egress serine protease SUB1

Lidumniece, E.; Withers-Martinez, C.; Hackett, F.; Collins, C. R.; Perrin, A. J.; Koussis, K.; Bisson, C.; Blackman, M. J.; Jirgensons, A. Proc. Natl. Acad. Sci. U.S.A., 2021, 118, e2022696118. DOI:10.1073/pnas.2022696118



68. Friedel–Crafts Alkylation with Carbenium Ions Generated by Electrochemical Oxidation of Stannylmethyl Ethers

Lielpetere, A.; Jirgensons, A., Eur. J. Org. Chem., 2020, 29, 4510-4516. DOI:10.1002/ejoc.202000568

Graphical abstract: Johnson–Corey–Chaykovsky fluorocyclopropanation of double activated alkenes: scope and limitations



67. 2-Aminoquinazolines by Chan–Evans–Lam Coupling of Guanidines with (2-Formylphenyl)boronic Acids

Solomin, V. V.; Seins, A.; Jirgensons, A., Synlett, 2020, 31, 1507-1510. DOI:10.1055/s-0040-1707080

Graphical abstract: Johnson–Corey–Chaykovsky fluorocyclopropanation of double activated alkenes: scope and limitations


66. Synthesis of 2-Aminopyridopyrimidinones and Their Plasmepsin I, II, IV Inhibition Potency

Rasina, D.; Stakanovs, G.; Kanepe-Lapsa, I.; Bobrovs, R.; Jirgensons, A., Chem. Heterocycl. Compd., 2020, 56, 786-792. DOI:10.1007/s10593-020-02731-3

Graphical abstract: Johnson–Corey–Chaykovsky fluorocyclopropanation of double activated alkenes: scope and limitations


65. A Concise Bioinspired Semisynthesis of Rumphellaones A–C and Their C-8 Epimers from β-Caryophyllene

Stakanovs, G.; Mishnev, A.; Rasina, D.; Jirgensons, A., J. Nat. Prod. 2020, 83, 6, 2004-2009. DOI:10.1021/acs.jnatprod.0c00403

Graphical abstract: Johnson–Corey–Chaykovsky fluorocyclopropanation of double activated alkenes: scope and limitations


64. Exploiting Structural Dynamics to Design Open-Flap Inhibitors of Malarial Aspartic Proteases

Bobrovs, R.; Jaudzems, K.; Jirgensons, A. J. Med. Chem., 2019, 62, 20, 8931-8950. DOI:10.1021/acs.jmedchem.9b00184




63. A Novel Collaborative Approach to Facilitate Chemical Biology

Brennecke, P.; Rasina, D.; Aubi, O.; Herzog, K.; Landskron, J.; Cautain, B.; Vicente, F.; Quintana, J.; Mestres, J.; Stechmann, B.; Ellinger, B.; Brea, J; Kolanowski, J. L.; Pilarski, R.; Orzaez, M.; Pineda-Lucena, A.; Laraia, L.; Nami, F.; Zielenkiewicz, P.; Paruch, K.; Hansen, E.; Von Kries, J. P.; Neuenschwander, M.; Specker, E.; Bartunek, P.; Simova, S.; Leśnikowski, Z.; Krauss, S.; Lehtiö, L.; Bilitewski, U.; Brönstrup, M.; Taskén, K.; Jirgensons, A.; Lickert, H.; Clausen, M. H.; Andersen, J. H.; Vicent, M. J.; Genilloud, O.; Martinez, A.; Nazaré, M.; Fecke, W.; Gribbon, P.
SLAS Discov., 2019, 24, 398–413. DOI:10.1177/2472555218816276



62. Amination of Carbenium Ions Generated by Directed Protonolysis of Cyclopropane

Skvorcova, M.; Lukasevics, T. L.; Jirgensons, A. J. Org. Chem., 2019 84, 3780-3792. DOI:10.1021/acs.joc.8b02576




61. Peptidomimetic Plasmepsin Inhibitors with Potent Anti-Malarial Activity and Selectivity Against Cathepsin D

Zogota, R.; Kinena, L.; Withers-Martinez, C.; Blackman, M.J.; Bobrovs, R.; Pantelejevs, T.; Kanepe-Lapsa, I.; Ozola, V.; Jaudzems, K.; Suna, E.; Jirgensons, A. Eur. J. Med. Chem., 2019, 163, 344-352. DOI:10.1016/j.ejmech.2018.11.068



60. Refining the Structure−Activity Relationships of 2-Phenylcyclopropane Carboxylic Acids as Inhibitors of O-Acetylserine Sulfhydrylase Isoforms

Magalhães, J.; Franko, N.; Annunziato, G.; Pieroni, M.; Benoni, R.; Nikitjuka, A.; Mozzarelli, A.; Bettati, S.; Karawajczyk, A.; Jirgensons, A.; Campanini, B.; Costantino, G. J. Enzyme Inhib. Med. Chem., 2019, 34, 31-43. DOI:10.1080/14756366.2018.1518959



59. Azole-Based Non-Peptidomimetic Plasmepsin Inhibitors

Kinena, L.; Leitis, G.; Kanepe-Lapsa, I.; Bobrovs, R.; Jaudzems, K.; Ozola, V.; Suna, E., Jirgensons, A. Arch. Pharm. Chem. Life Sci., 2018, 351, 1800151. DOI:10.1002/ardp.201800151



58. 2-Aminoquinazolin-4(3H)-one Based Plasmepsin Inhibitors with Improved Hydrophilicity and Selectivity

Rasina, D.; Stakanovs, G.; Borysov, O.V.; Pantelejevs, T.; Bobrovs, R.; Kanepe-Lapsa, I.; Tars, K.; Jaudzems, K.; Jirgensons, A. Biorg. Med. Chem., 2018, 26(9), 2488-2500. DOI:10.1016/j.bmc.2018.04.012



57. N-Leucinyl Benzenesulfonamides as Structurally Simplified Leucyl-tRNA Synthetase Inhibitors

Charlton, M.H.; Aleksis, R.; Saint-Leger, A.; Gupta, A; Loza, E.; , Ribas De Pouplana, L.;  Kaula, I.;  Gustina, D.; Madre, M.; Lola, D;  Jaudzems, K.;  Edmund, G.; Randall, C.P.; Kime, L.;  O’Neill, A.J.; Goessens, W.; Jirgensons, A.; Finn, P.W.  ACS Med. Chem. Lett.  2018, 9(2), 84-88. DOI:10.1021/acsmedchemlett.7b00374




56. Carbenium Ion Formation by Fragmentation of Electrochemically Generated Oxonium Ions

Lielpetere, A.; Jirgensons, A. Org. Biomol. Chem., 2018, 16, 5094-5096. DOI:10.1039/c8ob01339j



55. Inhibition of O-Acetylserine Sulfhydrylase by Fluoroalanine Derivatives

Franko, N.; Grammatoglou, K.; Campanini, B.; Costantino, G.; Jirgensons, A.; Mozzarelli, A. J. Enzyme Inhib. Med. Chem., 2018, 33, 1343-1351. DOI:10.1080/14756366.2018.1504040



54. Discovery of Novel Fragments Inhibiting O-Acetylserine Sulphhydrylase by Combining Scaffold Hopping and Ligand–Based Drug Design

Magalhães, J.; Franko, N.; Annunziato, G.; Welch, M.; Dolan, S.K.; Bruno, A.; Mozzarelli, A.; Armao, S.; Jirgensons, A.; Pieroni, M.; Costantino, G.; Campanini, B. J. Enzyme Inhib. Med. Chem., 2018, 33, 1444-1452. DOI:10.1080/14756366.2018.1512596



53. The Ritter Reaction for the Synthesis of Heterocycles (Minireview)

Bolsakova, J.; Jirgensons, A. Chem. Heterocycl. Compd., 2017, 53(11), 1167-1177. DOI:10.1007/s10593-018-2189-y



52. 1-Amino-1-hydroxymethylcyclobutane Derivatives via Intramolecular Amination of Nonclassical Cyclopropylmethyl Cation

Skvorcova, M., Grigorjeva, L., Jirgensons, A. Chem. Heterocycl. Compd., 2017, 53(9), 989-996. DOI:10.1007/s10593-017-2162-1



51. Amide-Group-Directed Protonolysis of Cyclopropane: An Approach to 2,2-Disubstituted Pyrrolidines

Skvorcova, M.; Jirgensons, A. Org. Lett., 2017, 19, 2478-2481. DOI:10.1021/acs.orglett.7b00584




50. N-Sulfonylcarboxamide as an Oxidizing Directing Group for Ruthenium-Catalyzed C–H Activation/Annulation

Petrova, E.; Rasina, D.;  Jirgensons, A. Eur. J. Org. Chem., 2017, 1773-1779. DOI:10.1002/ejoc.201601582

49. Intramolecular Cyclopropylmethylation via Non-Classical Carbocations

Skvorcova, M.; Jirgensons, A. Org. Biomol. Chem., 2017, 15, 6909-6912. DOI:10.1039/C7OB01721A



48. C-Quaternary Alkynyl Glycinols via the Ritter Reaction of Cobalt Complexed Alkynyl Glycols

Grammatoglou, K.; Bolsakova, J.; Jirgensons, A. RSC Adv., 2017, 7, 27530-27537. DOI:10.1039/C7RA03965D



47. Allylic Amination via Acid Catalyzed Leaving Group Activation

Skvorcova, M.; Jirgensons, A. Curr. Green Chem., 2016, 3(2), 145-159. DOI:10.2174/2213346103666160905101423



46. Evaluation of the Characteristics of Leucyl-tRNA Synthetase (LeuRS) Inhibitor AN3365 in Combination with Different Antibiotic Classes

Monteferrante, C.G.; Jirgensons, A.; Varik, V.; Hauryliuk, V.; Goessens, W.H.F.; Hays, J.P. Eur. J. Clin. Microbiol. Infect. Dis., 2016, 35, 1857-1864. DOI:10.1007/s10096-016-2738-1



45. Targeting Multiple Aminoacyl-tRNA Synthetases Overcomes the Resistance Liabilities Associated with Antibacterial Inhibitors Acting on a Single Such Enzyme

Randall, C.; Rasina, D.; Jirgensons, A.; O’Neill, A.J. Antimicrob. Agents Chemother., 2016, 60(10), 6359-6361. DOI:10.1128/AAC.00674-16



44. Crystal Structure of Plasmodium Falciparum Proplasmepsin IV: the Plasticity of Proplasmepsins

Recacha, R.; Jaudzems, K.; Akopjana, I.; Jirgensons, A.; Tars, K.
Acta Cryst., 2016, F72, 659-666. DOI:10.1107/S2053230X16011663



43. A Polymorphism in LeuS Confers Reduced Susceptibility to GSK2251052 in a Clinical Isolate of Staphylococcus Aureus

Gupta, A.; Monteferrante, C.; Rasina, D.; Leitis, G.; Randall, C.P.; Tomlinson, J.H. Jirgensons, A.; Goessens, W.H.F.; Hays, J. P.; O’Neill, A.J. Antimicrob. Agents Chemother., 2016, 60(5), 3219-3221. DOI:10.1128/AAC.02940-15



42. Fragment-Based Discovery of 2-Aminoquinazolin-4(3H)-ones as Novel Class Nonpeptidomimetic Inhibitors of the Plasmepsins I, II, and IV

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. J. Med. Chem., 2016, 59, 374–387. DOI:10.1021/acs.jmedchem.5b01558




41. Synthesis of α‐Ethynyl Glycines (Microreview)

Bolsakova, J.; Jirgensons, A. Eur. J. Org. Chem., 2016, 27, 4591-4602. DOI:10.1002/ejoc.201600253



40. Synthesis of Alkynyl‐Glycinols by Lewis Acid Catalyzed Propargylic Substitution of Bis‐Imidates

Sirotkina, J.; Grigorjeva, L.; Jirgensons, A. Eur. J. Org. Chem. 2015, 6900-6908. DOI: 10.1002/ejoc.201500937



39. Synthesis and Biological Evaluation of Aziridin-1-yl Oxime-Based Vorinostat Analogs as Anticancer Agents

Nikitjuka, A.; Shestakova, I.; Romanchikova, N.; Jirgensons A. Chem. Heterocycl. Compd., 2015, 51(7), 647-657. DOI:10.1007/s10593-015-1752-z



38. Tetrahydro-1,3-oxazepines via Intramolecular Amination of Cyclopropylmethyl Cation

Skvorcova, M.; Grigorjeva, L.; Jirgensons, A. Org. Lett., 2015, 17, 2902–2904. DOI:10.1021/acs.orglett.5b01014




37. 2-Vinyl Threoninol Derivatives via Acid-Catalyzed Allylic Substitution of Bisimidates

Kumar, V.; Klimovica, K.;  Rasina, D.; Jirgensons A. J. Org. Chem., 2015, 80, 5934–5943. DOI:10.1021/acs.joc.5b00529




36. Unsaturated syn– and anti-1,2-Amino Alcohols by Cyclization of Allylic Bis-trichloroacetimidates. Stereoselectivity Dependence on Substrate Configuration

Grigorjeva,  L.;  Kinens, A.;  Jirgensons,  A. J. Org. Chem., 2015, 80, 920–927. DOI:10.1021/jo502404y




35. Quinoxaline-Based Inhibitors of Malarial Protease PfSUB1

Kher, S.S.; Penzo, M.; Fulle, S.; Ebejer,  J.P.;  Finn, P.W. ; Blackman, M.J.; Jirgensons, A. Chem. Heterocycl. Compd., 2015, 50, 1457-1463. DOI:10.1007/s10593-014-1610-4

34. Structures of Plasmepsin II from Plasmodium Falciparum in Complex with Two Hydroxyethylamine-Based Inhibitors

Recacha, R.; Leitans, J.; Akopjana, I.; Aprupe, L.; Trapencieris, P.; Jaudzems, K.; Jirgensons, A.; Tars, K. Acta Cryst. 2015, F71, 1531-1539. DOI:10.1107/S2053230X15022049



33. Methylprenyl and Prenyl Protection for Sulfonamides

Nikitjuka, A.;  Nekrasova, A.; Jirgensons A. Synlett, 2015,  26, 183-186. DOI:10.1055/s-0034-1379428



32. Substrate Derived Peptidic α-Ketoamides as Inhibitors of the Malarial Protease PfSUB1

Kher, S.S.; Penzo, M.; Fulle, S.; Finn, P.W. ; Blackman, M.J.; Jirgensons, A. Bioorg. Med. Chem. Lett.,  2014, 24(18), 4486-4489. DOI:10.1016/j.bmcl.2014.07.086



31. Semisynthesis of Libiguin A and Its Analogues by Trans-Lactonization of Phragmalin

Grigorjeva, L.; Liepinsh, E.; Razafimahefa, S.; Yahorau, A.; Yahorava, S.; Rasoanaivo, P.; Jirgensons, A.; Wikberg, J.E.S. J. Org. Chem., 2014, 79(9), 4148–4153. DOI:10.1021/jo500318w




30. Plasmepsin Inhibitory Activity and Structure-Guided Optimization of a Potent Hydroxyethylamine-Based Antimalarial Hit

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. ACS Med. Chem. Lett., 2014, 5(4), 373–377. DOI:10.1021/ml4004952




29. Synthesis of β-Amino-α-ketoamides (Review)

Kher, S.S.; Jirgensons, A. Curr. Org. Chem., 2014, 18, 2240-2269. DOI:10.2174/1385272819666140818223225



28. Synthesis, Chemical and Biological Properties of Aziridine-1-carbaldehyde Oximes (Minireview)

Nikitjuka, A.; Jirgensons, A. Chem. Heterocycl. Compd., 2014, 49, 1544-1559. Dedicated to Professor Jānis Stradiņš on the occasion of his 80 anniversary. DOI:10.1007/s10593-014-1407-5



27. Unsaturated Amino Alcohols via Cyclization of Allylic Bistrichloroacetimidates

Jirgensons, A.; Grigorjeva, L.; Maleckis, A.; Klimovica, K. Synlett, 2013, 24(18), 2345-2349. DOI:10.1055/s-0033-1338977



26. Synthesis of 5-Substituted 3-Mercapto-1,2,4-triazoles via Suzuki–Miyaura Reaction

Katkevica, S.; Salun, P.; Jirgensons, A. Tetrahedron Lett., 2013, 54, 4524–4525. DOI:10.1016/j.tetlet.2013.06.067



25. Synthesis of Hydroxamic Acids by Using the Acid Labile O-2-Methylprenyl Protecting Group

Nikitjuka, A.; Jirgensons, A. Synlett, 2012, 23, 2972-2974. DOI:10.1055/s-0032-1317687



24. Synthesis of Cyclic N-Tosyliminocarbonates by Lewis Acid Catalysed Allylic Substitution of Trichloroacetimidates

Grigorjeva, L.; Jirgensons, A. Eur. J. Org. Chem., 2012, 27, 5307–5316. DOI:10.1002/ejoc.201200378



23. Plasmodium Subtilisin-like Protease 1 (SUB1): Insights into the Active-Site Structure, Specificity and Function of a Pan-Malaria Drug Target

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. Int. J. Parasitol., 2012, 42, 597-612. DOI:10.1016/j.ijpara.2012.04.005



22. Novel Synthesis of 2-Trichloromethyl-4-vinyl-oxazoline and its Derivatization by Ring Cleavage Reactions

Grigorjeva, L.; Maleckis, A.; Klimovica, K.; Skvorcova, M.; Ivdra, N.; Leitis, G.; Jirgensons, A. Chem. Heterocycl. Compd., 2012, 48, 919-924. Dedicated to professor Ivars Kalvinsh on the occasion of his 65th birthday. DOI:10.1007/s10593-012-1077-0



21. C-Quaternary Vinylglycinols by Metal-Catalysed Cyclization of Allylic Bistrichloroacetimidates

Klimovica, K.; Grigorjeva, L.; Maleckis, A.; Popelis, J.; Jirgensons, A. Synlett, 2011, 2849-2851. DOI:10.1055/s-0031-1289537



20. Lewis Acid Catalyzed Intramolecular Allylic Substitution of Bis(trichloroacetimidates): A Versatile Approach to Racemic Unsaturated Amino Acids

Grigorjeva, L.; Jirgensons, A. Eur. J. Org. Chem., 2011, 2421–2425. DOI:10.1002/ejoc.201100060



19. Catalytic Enantioselective Synthesis of 4-Vinyl-2-trichloromethyloxazoline: An Access to Enantioenriched Vinylglycinol Surrogate

Maleckis, A.; Klimovica, K.; Jirgensons, A. J. Org. Chem., 2010, 75, 7897-7900. DOI:10.1021/jo101781y




18. Synthesis of Hydroxamic Acids by Activation of Carboxylic Acids with N,N’-Carbonyldiimidazole: Exploring the Efficiency of the Method

Usachova, N.; Leitis, G.; Jirgensons, A.; Kalvinsh I. Synthetic Comm., 2010, 40, 927–935. DOI:10.1080/00397910903026723



17. Cyclization of Trichloroacetimidates by Olefin Aminopalladation β‐Heteroatom Elimination

Maleckis, A.; Jaunzeme, I.; Jirgensons, A. Eur. J. Org. Chem., 2009, 6407–6412. DOI:10.1002/ejoc.200900917



16. Synthesis of Novel [1-Aziridinyl-(hydroxyimino)methyl]arenes and Their Cytotoxic Activity

Grigorjeva, А.; Jirgensons, A.; Domracheva, I.; Jaschenko, E.; Shestakova, I.; Andrianov, V.; Kalvinsh, I. Chem. Heterocycl. Compd., 2009, 45, 203-213. DOI:10.1007/s10593-009-0245-3



15. Identification of GCP II Inhibitors Based on 4-Arylmethyl-3-(4-carboxyphenyl)-5-hydroxyisoxazole Scaffold

Teus, M.; Jirgensons, A.; Dambrova, M.; Mezhapuke, R.; Parsons, C.G.; Danysz, W. Lett. Drug Des. Discov., 2009, 6, 29-32. DOI:10.2174/157018009787158544



14. Ether-Directed Diastereoselectivity in Catalysed Overman Rearrangement: Comparative Studies of Metal Catalysts

Jaunzeme, I.; Jirgensons, A. Tetrahedron, 2008, 64, 5794-5799. DOI:10.1016/j.tet.2008.03.099



13. Virtual Screening for Selective Allosteric mGluR1 Antagonists and Structure-Activity Relationship Investigations for Coumarine Derivatives

Noeske, T.; Jirgensons, A.; Starchenkovs, I.; Renner, S.; Jaunzeme, I.; Trifanova, D.; Hechenberger, M.; Bauer, T.; Kauss, V.; Parsons, C.G.; Schneider, G.; Weil, T. Chem. Med. Chem., 2007, 2, 1763-1773. DOI:10.1002/cmdc.200700151



12. A Novel Class of Amino-alkylcyclohexanes as Uncompetitive, Fast, Voltage-Dependent, N-Methyl-D-aspartate (NMDA) Receptor Antagonists – in vitro Characterization

Gilling, K.; Jatzke, C.; Wollenburg, C.; Vanejevs, M.; Kauss, V.; Jirgensons, A.; Parsons, C.G. J. Neural. Transm., 2007, 114, 1529-1537. DOI:10.1007/s00702-007-0792-7



11. Synthesis and GCP II Inhibitory Activity of 4[4-(3-Bromobenzyl)-5-hydroxyisoxazol-3-yl]benzoic Acid Heterocyclic Analogs

Teus, M.; Jirgensons, A.; Dambrova, M.; Mezhapuke, R. Chem. Heterocycl. Compd., 2007, 43, 1440-1444. DOI:10.1007/s10593-007-0222-7



10. Effects of NAAG Peptidase Inhibitor 2-PMPA in Model Chronic Pain – Relation to Brain Concentration

Nagel, J.; Belozertseva, I.; Greco, S.; Kashkin, V.; Malyshkin, A.; Jirgensons, A.; Shekunova, E.; Eilbacher, B.; Bespalov, A.; Danysz, W. Neuropharmacology, 2006, 51, 1163-1171. DOI:10.1016/j.neuropharm.2006.07.018



9. Diastereoselectivity in the Overman Rearrangement of O-Cyclohexylideneethylimidates

Jaunzeme, I.; Jirgensons, A.; Kauss, V.; Liepins, E. Tetrahedron Lett., 2006, 3885-3887. DOI:10.1016/j.tetlet.2006.03.174



8. Novel Catalysts for Overman Rearrangement

Jaunzeme, I.; Jirgensons, A. Synlett, 2005, 2984-2986. DOI:10.1055/s-2005-918952



7. Conformationally Constrained Amino Acids: Enantiodivergent Synthesis of All Four Stereoisomers of 2-(Tetrahydrofuran-2-yl)glycine

Jirgensons, A.; Marinozzi, M.; Pellicciari R. Tetrahedron, 2005, 61, 373-377. DOI:10.1016/j.tet.2004.10.091



6. The Synthesis of Potential Neramexane Metabolites: Cis- and Trans-3-amino-1,3,5,5-tetramethylcyclohexane Carboxylic Acids

Trifanova, D.; Trifonova, M.; Jirgensons, A.; Kauss, V.; Pugovich, O.; Kalvinsh, I.; Quack, G. Tetrahedron Lett., 2004, 45, 8145-8147. DOI:10.1016/j.tetlet.2004.09.047



5. Amino-Alkyl-Cyclohexanes as a Novel Class of Uncompetitive NMDA Receptor Antagonists

Danysz, W.; Parsons, C.G.; Jirgensons, A.; Kauss, V.; Tillner, J. Curr. Pharm. Design, 2002, 8, 835-843. DOI:10.2174/1381612024607117



4. A Practical Synthesis of tert-Alkylamines via the Ritter Reaction with Chloroacetonitrile

Jirgensons, A.; Kauss, V.; Kalvinsh, I.; Gold, M.R. Synthesis, 2000, 1709-1712DOI:10.1055/s-2000-8208



3. Synthesis and Structure – Affinity Relationships of 1,3,5-Alkylsubstituted Cyclohexylamines Binding at NMDA Receptor PCP Site

Jirgensons, A.; Kauss, V.; Kalvinsh, I.; Gold, M.R.; Danysz, W.; Parsons, C.G.; Quack, G. Eur. J. Med. Chem., 2000, 35, 555-565. DOI:10.1016/S02235234(00)00153-7



2. The Synthesis of 3-Amino-3-methylbicyclo[3.3.1]nonanes. Endo-Selectivity in the Ritter Reaction of 1,3,5,7α -Tetramethylbicyclo[3.3.1]nonan-3-ol

Jirgensons, A.; Kauss, V.; Mishnev, A.F.; Kalvinsh, I. J. Chem. Soc., Perkin Trans. 1, 1999, 0, 3527-3530. DOI:10.1039/A904394B



1. A Convenient Reagent for N-Hydroxyguanylation

Jirgensons, A.; Kums, I.; Kauss, V.; Kalvinsh, I. Synth. Comm., 1997, 27, 315-322. DOI:10.1080/00397919708005034




Patent Applications: 20

WIPO: Aigars Jirgensons