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Page 1
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
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
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
Fragment-Based Discovery of Dual JC Virus and BK Virus Helicase Inhibitors.
Bonafoux D, Nanthakumar S, Bandarage UK, Memmott C, Lowe D, Aronov AM, Bhisetti GR, Bonanno KC, Coll J, Leeman J, Lepre CA, Lu F, Perola E, Rijnbrand R, Taylor WP, Wilson D, Zhou Y, Zwahlen J, Ter Haar E. Bonafoux D, et al. Among authors: perola e. J Med Chem. 2016 Aug 11;59(15):7138-51. doi: 10.1021/acs.jmedchem.6b00486. Epub 2016 Jul 20. J Med Chem. 2016. PMID: 27385654
Discovery of Novel, Orally Bioavailable β-Amino Acid Azaindole Inhibitors of Influenza PB2.
Farmer LJ, Clark MP, Boyd MJ, Perola E, Jones SM, Tsai A, Jacobs MD, Bandarage UK, Ledeboer MW, Wang T, Deng H, Ledford B, Gu W, Duffy JP, Bethiel RS, Shannon D, Byrn RA, Leeman JR, Rijnbrand R, Bennett HB, O'Brien C, Memmott C, Nti-Addae K, Bennani YL, Charifson PS. Farmer LJ, et al. Among authors: perola e. ACS Med Chem Lett. 2017 Jan 20;8(2):256-260. doi: 10.1021/acsmedchemlett.6b00486. eCollection 2017 Feb 9. ACS Med Chem Lett. 2017. PMID: 28197322 Free PMC article.
36 results