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Page 1
Discovery and Optimization of Pyrazole Amides as Inhibitors of ELOVL1.
Come JH, Senter TJ, Clark MP, Court JJ, Gale-Day Z, Gu W, Krueger E, Liang J, Morris M, Nanthakumar S, O'Dowd H, Maltais F, Iyer G, Andreassi J, Boucher C, Considine T, Moody CS, Taylor W, Mohanty AK, Huang Y, Zuccola H, Coll J, Bonanno KC, Gagnon KJ, Gan L, Lu F, Gao H, Chakilam A, Engtrakul J, Song B, Crawford D, Doyle E, Kramer T, Vought B, Phillips J, Kemper R, Sanders M, Swett R, Furey B, Winquist R, Bunnage ME, Jackson KL, Charifson PS, Magavi SS. Come JH, et al. Among authors: charifson ps. J Med Chem. 2021 Dec 23;64(24):17753-17776. doi: 10.1021/acs.jmedchem.1c00944. Epub 2021 Nov 8. J Med Chem. 2021. PMID: 34748351
Discovery of Novel, Orally Bioavailable Pyrimidine Ether-Based Inhibitors of ELOVL1.
Boyd MJ, Collier PN, Clark MP, Deng H, Kesavan S, Ronkin SM, Waal N, Wang J, Cao J, Li P, Come J, Davies I, Duffy JP, Cochran JE, Court JJ, Chandupatla K, Jackson KL, Maltais F, O'Dowd H, Boucher C, Considine T, Taylor WP, Gao H, Chakilam A, Engtrakul J, Crawford D, Doyle E, Phillips J, Kemper R, Swett R, Empfield J, Bunnage ME, Charifson PS, Magavi SS. Boyd MJ, et al. Among authors: charifson ps. J Med Chem. 2021 Dec 23;64(24):17777-17794. doi: 10.1021/acs.jmedchem.1c00948. Epub 2021 Dec 6. J Med Chem. 2021. PMID: 34871500
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: charifson ps. 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: charifson ps. 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: charifson ps. 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: charifson ps. J Med Chem. 2014 Nov 13;57(21):8792-816. doi: 10.1021/jm500563g. Epub 2014 Oct 28. J Med Chem. 2014. PMID: 25317480
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: charifson ps. 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
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: charifson ps. 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 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: charifson ps. 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.
Novel 2-Substituted 7-Azaindole and 7-Azaindazole Analogues as Potential Antiviral Agents for the Treatment of Influenza.
Bandarage UK, Clark MP, Perola E, Gao H, Jacobs MD, Tsai A, Gillespie J, Kennedy JM, Maltais F, Ledeboer MW, Davies I, Gu W, Byrn RA, Nti Addae K, Bennett H, Leeman JR, Jones SM, O'Brien C, Memmott C, Bennani Y, Charifson PS. Bandarage UK, et al. Among authors: charifson ps. ACS Med Chem Lett. 2017 Jan 18;8(2):261-265. doi: 10.1021/acsmedchemlett.6b00487. eCollection 2017 Feb 9. ACS Med Chem Lett. 2017. PMID: 28197323 Free PMC article.
50 results