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Items: 32

1.

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

Bobrovs R, Jaudzems K, Jirgensons A.

J Med Chem. 2019 Oct 24;62(20):8931-8950. doi: 10.1021/acs.jmedchem.9b00184. Epub 2019 May 16.

PMID:
31062983
2.

Amination of Carbenium Ions Generated by Directed Protonolysis of Cyclopropane.

Skvorcova M, Lukasevics LT, Jirgensons A.

J Org Chem. 2019 Apr 5;84(7):3780-3792. doi: 10.1021/acs.joc.8b02576. Epub 2019 Mar 18.

PMID:
30854858
3.

EU-OPENSCREEN: 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 JL, Pilarski R, Orzaez M, Pineda-Lucena A, Laraia L, Nami F, Zielenkiewicz P, Paruch K, Hansen E, von Kries JP, 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 MH, Andersen JH, Vicent MJ, Genilloud O, Martinez A, Nazaré M, Fecke W, Gribbon P.

SLAS Discov. 2019 Mar;24(3):398-413. doi: 10.1177/2472555218816276. Epub 2019 Jan 7.

4.

Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D.

Zogota R, Kinena L, Withers-Martinez C, Blackman MJ, Bobrovs R, Pantelejevs T, Kanepe-Lapsa I, Ozola V, Jaudzems K, Suna E, Jirgensons A.

Eur J Med Chem. 2019 Feb 1;163:344-352. doi: 10.1016/j.ejmech.2018.11.068. Epub 2018 Nov 29.

5.

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 Dec;34(1):31-43. doi: 10.1080/14756366.2018.1518959.

6.

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 Dec;33(1):1343-1351. doi: 10.1080/14756366.2018.1504040.

7.

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 SK, Bruno A, Mozzarelli A, Armao S, Jirgensons A, Pieroni M, Costantino G, Campanini B.

J Enzyme Inhib Med Chem. 2018 Dec;33(1):1444-1452. doi: 10.1080/14756366.2018.1512596.

8.

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 (Weinheim). 2018 Sep;351(9):e1800151. doi: 10.1002/ardp.201800151. Epub 2018 Jul 31.

PMID:
30063266
9.

Carbenium ion formation by fragmentation of electrochemically generated oxonium ions.

Lielpetere A, Jirgensons A.

Org Biomol Chem. 2018 Jul 18;16(28):5094-5096. doi: 10.1039/c8ob01339j.

PMID:
29971288
10.

2-Aminoquinazolin-4(3H)-one based plasmepsin inhibitors with improved hydrophilicity and selectivity.

Rasina D, Stakanovs G, Borysov OV, Pantelejevs T, Bobrovs R, Kanepe-Lapsa I, Tars K, Jaudzems K, Jirgensons A.

Bioorg Med Chem. 2018 May 15;26(9):2488-2500. doi: 10.1016/j.bmc.2018.04.012. Epub 2018 Apr 5.

PMID:
29636223
11.

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

Charlton MH, 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 CP, Kime L, O'Neill AJ, Goessens W, Jirgensons A, Finn PW.

ACS Med Chem Lett. 2018 Jan 18;9(2):84-88. doi: 10.1021/acsmedchemlett.7b00374. eCollection 2018 Feb 8.

12.

Intramolecular cyclopropylmethylation via non-classical carbocations.

Skvorcova M, Jirgensons A.

Org Biomol Chem. 2017 Aug 23;15(33):6909-6912. doi: 10.1039/c7ob01721a.

PMID:
28792551
13.

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

Skvorcova M, Jirgensons A.

Org Lett. 2017 May 19;19(10):2478-2481. doi: 10.1021/acs.orglett.7b00584. Epub 2017 Apr 28.

PMID:
28453291
14.

Crystal structure of Plasmodium falciparum proplasmepsin IV: the plasticity of proplasmepsins.

Recacha R, Jaudzems K, Akopjana I, Jirgensons A, Tars K.

Acta Crystallogr F Struct Biol Commun. 2016 Sep;72(Pt 9):659-66. doi: 10.1107/S2053230X16011663. Epub 2016 Aug 9.

15.

Evaluation of the characteristics of leucyl-tRNA synthetase (LeuRS) inhibitor AN3365 in combination with different antibiotic classes.

Monteferrante CG, Jirgensons A, Varik V, Hauryliuk V, Goessens WH, Hays JP.

Eur J Clin Microbiol Infect Dis. 2016 Nov;35(11):1857-1864. Epub 2016 Aug 9.

16.

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

Randall CP, Rasina D, Jirgensons A, O'Neill AJ.

Antimicrob Agents Chemother. 2016 Sep 23;60(10):6359-61. doi: 10.1128/AAC.00674-16. Print 2016 Oct.

17.

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 CP, Tomlinson JH, Jirgensons A, Goessens WH, Hays JP, O'Neill AJ.

Antimicrob Agents Chemother. 2016 Apr 22;60(5):3219-21. doi: 10.1128/AAC.02940-15. Print 2016 May.

18.

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 OV, Kanepe-Lapsa I, Domraceva I, Pantelejevs T, Tars K, Blackman MJ, Jaudzems K, Jirgensons A.

J Med Chem. 2016 Jan 14;59(1):374-87. doi: 10.1021/acs.jmedchem.5b01558. Epub 2015 Dec 23.

PMID:
26670264
19.

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 Crystallogr F Struct Biol Commun. 2015 Dec;71(Pt 12):1531-9. doi: 10.1107/S2053230X15022049. Epub 2015 Nov 27.

20.

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

Skvorcova M, Grigorjeva L, Jirgensons A.

Org Lett. 2015 Jun 19;17(12):2902-4. doi: 10.1021/acs.orglett.5b01014. Epub 2015 Jun 3.

PMID:
26039677
21.

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

Kumar V, Klimovica K, Rasina D, Jirgensons A.

J Org Chem. 2015 Jun 5;80(11):5934-43. doi: 10.1021/acs.joc.5b00529. Epub 2015 May 18.

PMID:
25941908
22.

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 Jan 16;80(2):920-7. doi: 10.1021/jo502404y. Epub 2014 Dec 22.

PMID:
25484278
23.

Substrate derived peptidic α-ketoamides as inhibitors of the malarial protease PfSUB1.

Kher SS, Penzo M, Fulle S, Finn PW, Blackman MJ, Jirgensons A.

Bioorg Med Chem Lett. 2014 Sep 15;24(18):4486-4489. doi: 10.1016/j.bmcl.2014.07.086. Epub 2014 Aug 7.

24.

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 MJ, Jirgensons A.

ACS Med Chem Lett. 2014 Jan 13;5(4):373-7. doi: 10.1021/ml4004952. eCollection 2014 Apr 10.

25.

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 JE.

J Org Chem. 2014 May 2;79(9):4148-53. doi: 10.1021/jo500318w. Epub 2014 Apr 21.

PMID:
24716657
26.

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 JP, Koussis K, Hackett F, Jirgensons A, Finn P, Blackman MJ.

Int J Parasitol. 2012 May 15;42(6):597-612. doi: 10.1016/j.ijpara.2012.04.005. Epub 2012 Apr 27.

27.

Catalytic enantioselective synthesis of 4-vinyl-2-trichloromethyloxazoline: an access to enantioenriched vinylglycinol surrogate.

Maleckis A, Klimovica K, Jirgensons A.

J Org Chem. 2010 Nov 19;75(22):7897-900. doi: 10.1021/jo101781y. Epub 2010 Oct 25.

PMID:
20973520
28.

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 CG, Schneider G, Weil T.

ChemMedChem. 2007 Dec;2(12):1763-73.

PMID:
17868161
29.

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 CG.

J Neural Transm (Vienna). 2007;114(12):1529-37. Epub 2007 Aug 31.

PMID:
17728997
30.

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 Dec;51(7-8):1163-71. Epub 2006 Aug 22.

PMID:
16926034
31.

Amino-alkyl-cyclohexanes as a novel class of uncompetitive NMDA receptor antagonists.

Danysz W, Parsons CG, Jirgensons A, Kauss V, Tillner J.

Curr Pharm Des. 2002;8(10):835-43. Review.

PMID:
11945134
32.

Synthesis and structure-affinity relationships of 1,3, 5-alkylsubstituted cyclohexylamines binding at NMDA receptor PCP site.

Jirgensons A, Kauss V, Kalvinsh I, Gold MR, Danysz W, Parsons CG, Quack G.

Eur J Med Chem. 2000 Jun;35(6):555-65.

PMID:
10906408

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