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Page 1
Benzimidazole-containing HCV NS5A inhibitors: effect of 4-substituted pyrrolidines in balancing genotype 1a and 1b potency.
Henderson JA, Bilimoria D, Bubenik M, Cadilhac C, Cottrell KM, Dietrich E, Denis F, Ewing N, Falardeau G, Giroux S, Grey R Jr, L'Heureux L, Liu B, Mani N, Morris M, Nicolas O, Pereira OZ, Poisson C, Govinda Rao B, Reddy TJ, Selliah S, Shawgo RS, Vaillancourt L, Wang J, Yannopoulos CG, Chauret N, Berlioz-Seux F, Chan LC, Das SK, Grillot AL, Bennani YL, Maxwell JP. Henderson JA, et al. Among authors: grillot al. Bioorg Med Chem Lett. 2015 Feb 15;25(4):944-7. doi: 10.1016/j.bmcl.2014.12.045. Epub 2014 Dec 20. Bioorg Med Chem Lett. 2015. PMID: 25577041
Discovery of Thienoimidazole-Based HCV NS5A Genotype 1a and 1b Inhibitors.
Giroux S, Xu J, Reddy TJ, Morris M, Cottrell KM, Cadilhac C, Henderson JA, Nicolas O, Bilimoria D, Denis F, Mani N, Ewing N, Shawgo R, L'Heureux L, Selliah S, Chan L, Chauret N, Berlioz-Seux F, Namchuk MN, Grillot AL, Bennani YL, Das SK, Maxwell JP. Giroux S, et al. Among authors: grillot al. ACS Med Chem Lett. 2013 Jan 27;5(3):240-3. doi: 10.1021/ml300461f. eCollection 2014 Mar 13. ACS Med Chem Lett. 2013. PMID: 24900811 Free PMC article.
Synthesis and evaluation of NS5A inhibitors containing diverse heteroaromatic cores.
Henderson JA, Bilimoria D, Bubenik M, Cadilhac C, Cottrell KM, Denis F, Dietrich E, Ewing N, Falardeau G, Giroux S, L'Heureux L, Liu B, Mani N, Morris M, Nicolas O, Pereira OZ, Poisson C, Reddy TJ, Selliah S, Shawgo RS, Vaillancourt L, Wang J, Xu J, Chauret N, Berlioz-Seux F, Chan LC, Das SK, Grillot AL, Bennani YL, Maxwell JP. Henderson JA, et al. Among authors: grillot al. Bioorg Med Chem Lett. 2015 Feb 15;25(4):948-51. doi: 10.1016/j.bmcl.2014.12.042. Epub 2014 Dec 22. Bioorg Med Chem Lett. 2015. PMID: 25577039
Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 1: C2-symmetric inhibitors with diyne and biphenyl linkers.
Giroux S, Bilimoria D, Cadilhac C, Cottrell KM, Denis F, Dietrich E, Ewing N, Henderson JA, L'Heureux L, Mani N, Morris M, Nicolas O, Reddy TJ, Selliah S, Shawgo RS, Xu J, Chauret N, Berlioz-Seux F, Chan LC, Das SK, Grillot AL, Bennani YL, Maxwell JP. Giroux S, et al. Among authors: grillot al. Bioorg Med Chem Lett. 2015 Feb 15;25(4):936-9. doi: 10.1016/j.bmcl.2014.12.046. Epub 2014 Dec 30. Bioorg Med Chem Lett. 2015. PMID: 25595681
Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 2: non-symmetric inhibitors with potent activity against genotype 1a and 1b.
Giroux S, Bilimoria D, Cadilhac C, Cottrell KM, Denis F, Dietrich E, Ewing N, Henderson JA, L'Heureux L, Mani N, Morris M, Nicolas O, Reddy TJ, Selliah S, Shawgo RS, Xu J, Chauret N, Berlioz-Seux F, Chan LC, Das SK, Grillot AL, Bennani YL, Maxwell JP. Giroux S, et al. Among authors: grillot al. Bioorg Med Chem Lett. 2015 Feb 15;25(4):940-3. doi: 10.1016/j.bmcl.2014.12.044. Epub 2014 Dec 29. Bioorg Med Chem Lett. 2015. PMID: 25597006
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
Perola E, Stamos D, Grillot AL, Ronkin S, Wang T, LeTiran A, Tang Q, Deininger DD, Liao Y, Tian SK, Drumm JE, Nicolau DP, Tessier PR, Mani N, Grossman TH, Charifson PS. Perola E, et al. Among authors: grillot al. Bioorg Med Chem Lett. 2014 May 1;24(9):2177-81. doi: 10.1016/j.bmcl.2014.03.022. Epub 2014 Mar 19. Bioorg Med Chem Lett. 2014. PMID: 24685546
Second-generation antibacterial benzimidazole ureas: discovery of a preclinical candidate with reduced metabolic liability.
Grillot AL, Le Tiran A, Shannon D, Krueger E, Liao Y, O'Dowd H, Tang Q, Ronkin S, Wang T, Waal N, Li P, Lauffer D, Sizensky E, Tanoury J, Perola E, Grossman TH, Doyle T, Hanzelka B, Jones S, Dixit V, Ewing N, Liao S, Boucher B, Jacobs M, Bennani Y, Charifson PS. Grillot AL, et al. J Med Chem. 2014 Nov 13;57(21):8792-816. doi: 10.1021/jm500563g. Epub 2014 Oct 28. J Med Chem. 2014. PMID: 25317480
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.
Charifson PS, Grillot AL, Grossman TH, Parsons JD, Badia M, Bellon S, Deininger DD, Drumm JE, Gross CH, LeTiran A, Liao Y, Mani N, Nicolau DP, Perola E, Ronkin S, Shannon D, Swenson LL, Tang Q, Tessier PR, Tian SK, Trudeau M, Wang T, Wei Y, Zhang H, Stamos D. Charifson PS, et al. Among authors: grillot al. J Med Chem. 2008 Sep 11;51(17):5243-63. doi: 10.1021/jm800318d. Epub 2008 Aug 9. J Med Chem. 2008. PMID: 18690678
Discovery and Characterization of a Water-Soluble Prodrug of a Dual Inhibitor of Bacterial DNA Gyrase and Topoisomerase IV.
O'Dowd H, Shannon DE, Chandupatla KR, Dixit V, Engtrakul JJ, Ye Z, Jones SM, O'Brien CF, Nicolau DP, Tessier PR, Crandon JL, Song B, Macikenas D, Hanzelka BL, Le Tiran A, Bennani YL, Charifson PS, Grillot AL. O'Dowd H, et al. Among authors: grillot al. ACS Med Chem Lett. 2015 Jun 22;6(7):822-6. doi: 10.1021/acsmedchemlett.5b00196. eCollection 2015 Jul 9. ACS Med Chem Lett. 2015. PMID: 26191374 Free PMC article.
Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase.
Ronkin SM, Badia M, Bellon S, Grillot AL, Gross CH, Grossman TH, Mani N, Parsons JD, Stamos D, Trudeau M, Wei Y, Charifson PS. Ronkin SM, et al. Among authors: grillot al. Bioorg Med Chem Lett. 2010 May 1;20(9):2828-31. doi: 10.1016/j.bmcl.2010.03.052. Epub 2010 Mar 15. Bioorg Med Chem Lett. 2010. PMID: 20356737
12 results