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Page 1
2-N-Arylthiazole inhibitors of Mycobacterium tuberculosis.
Clark MP, Wang T, Perola E, Deininger DD, Zuccola HJ, Jones SM, Gao H, VanderVen BC, Russell DG, Shoen CM, Cynamon MH, Thomson JA, Locher CP. Clark MP, et al. Among authors: perola e. Bioorg Med Chem Lett. 2017 Sep 1;27(17):3987-3991. doi: 10.1016/j.bmcl.2017.07.067. Epub 2017 Jul 27. Bioorg Med Chem Lett. 2017. PMID: 28778468
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. 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
A novel inhibitor of gyrase B is a potent drug candidate for treatment of tuberculosis and nontuberculosis mycobacterial infections.
Locher CP, Jones SM, Hanzelka BL, Perola E, Shoen CM, Cynamon MH, Ngwane AH, Wiid IJ, van Helden PD, Betoudji F, Nuermberger EL, Thomson JA. Locher CP, et al. Among authors: perola e. Antimicrob Agents Chemother. 2015 Mar;59(3):1455-65. doi: 10.1128/AAC.04347-14. Epub 2014 Dec 22. Antimicrob Agents Chemother. 2015. PMID: 25534737 Free PMC article.
Novel inhibitors of cholesterol degradation in Mycobacterium tuberculosis reveal how the bacterium's metabolism is constrained by the intracellular environment.
VanderVen BC, Fahey RJ, Lee W, Liu Y, Abramovitch RB, Memmott C, Crowe AM, Eltis LD, Perola E, Deininger DD, Wang T, Locher CP, Russell DG. VanderVen BC, et al. Among authors: perola e. PLoS Pathog. 2015 Feb 12;11(2):e1004679. doi: 10.1371/journal.ppat.1004679. eCollection 2015 Feb. PLoS Pathog. 2015. PMID: 25675247 Free PMC article.
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.
Boyd MJ, Bandarage UK, Bennett H, Byrn RR, Davies I, Gu W, Jacobs M, Ledeboer MW, Ledford B, Leeman JR, Perola E, Wang T, Bennani Y, Clark MP, Charifson PS. Boyd MJ, et al. Among authors: perola e. Bioorg Med Chem Lett. 2015 May 1;25(9):1990-4. doi: 10.1016/j.bmcl.2015.03.013. Epub 2015 Mar 14. Bioorg Med Chem Lett. 2015. PMID: 25827523
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: perola e. J Med Chem. 2008 Sep 11;51(17):5243-63. doi: 10.1021/jm800318d. Epub 2008 Aug 9. J Med Chem. 2008. PMID: 18690678
Design, synthesis and biological evaluation of potent NAD+-dependent DNA ligase inhibitors as potential antibacterial agents. Part 2: 4-amino-pyrido[2,3-d]pyrimidin-5(8H)-ones.
Wang T, Duncan L, Gu W, O'Dowd H, Wei Y, Perola E, Parsons J, Gross CH, Moody CS, Arends SJ, Charifson PS. Wang T, et al. Among authors: perola e. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3699-703. doi: 10.1016/j.bmcl.2012.04.038. Epub 2012 Apr 19. Bioorg Med Chem Lett. 2012. PMID: 22560470
Design, synthesis and biological evaluation of potent NAD+-dependent DNA ligase inhibitors as potential antibacterial agents. Part I: aminoalkoxypyrimidine carboxamides.
Gu W, Wang T, Maltais F, Ledford B, Kennedy J, Wei Y, Gross CH, Parsons J, Duncan L, Arends SJ, Moody C, Perola E, Green J, Charifson PS. Gu W, et al. Among authors: perola e. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3693-8. doi: 10.1016/j.bmcl.2012.04.037. Epub 2012 Apr 17. Bioorg Med Chem Lett. 2012. PMID: 22560473
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
Clark MP, Ledeboer MW, Davies I, Byrn RA, Jones SM, Perola E, Tsai A, Jacobs M, Nti-Addae K, Bandarage UK, Boyd MJ, Bethiel RS, Court JJ, Deng H, Duffy JP, Dorsch WA, Farmer LJ, Gao H, Gu W, Jackson K, Jacobs DH, Kennedy JM, Ledford B, Liang J, Maltais F, Murcko M, Wang T, Wannamaker MW, Bennett HB, Leeman JR, McNeil C, Taylor WP, Memmott C, Jiang M, Rijnbrand R, Bral C, Germann U, Nezami A, Zhang Y, Salituro FG, Bennani YL, Charifson PS. Clark MP, et al. Among authors: perola e. J Med Chem. 2014 Aug 14;57(15):6668-78. doi: 10.1021/jm5007275. Epub 2014 Jul 24. J Med Chem. 2014. PMID: 25019388
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. Among authors: perola e. J Med Chem. 2014 Nov 13;57(21):8792-816. doi: 10.1021/jm500563g. Epub 2014 Oct 28. J Med Chem. 2014. PMID: 25317480
35 results