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Page 1
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. J Med Chem. 2014 Aug 14;57(15):6668-78. doi: 10.1021/jm5007275. Epub 2014 Jul 24. J Med Chem. 2014. PMID: 25019388
Preclinical activity of VX-787, a first-in-class, orally bioavailable inhibitor of the influenza virus polymerase PB2 subunit.
Byrn RA, Jones SM, Bennett HB, Bral C, Clark MP, Jacobs MD, Kwong AD, Ledeboer MW, Leeman JR, McNeil CF, Murcko MA, Nezami A, Perola E, Rijnbrand R, Saxena K, Tsai AW, Zhou Y, Charifson PS. Byrn RA, et al. Among authors: clark mp. Antimicrob Agents Chemother. 2015 Mar;59(3):1569-82. doi: 10.1128/AAC.04623-14. Epub 2014 Dec 29. Antimicrob Agents Chemother. 2015. PMID: 25547360 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: clark mp. 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 Ranking System for Identifying Efficacious Anti-Influenza Virus PB2 Inhibitors.
Tsai AW, McNeil CF, Leeman JR, Bennett HB, Nti-Addae K, Huang C, Germann UA, Byrn RA, Berlioz-Seux F, Rijnbrand R, Clark MP, Charifson PS, Jones SM. Tsai AW, et al. Among authors: clark mp. Antimicrob Agents Chemother. 2015 Oct;59(10):6007-16. doi: 10.1128/AAC.00781-15. Epub 2015 Jul 13. Antimicrob Agents Chemother. 2015. PMID: 26169418 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: clark mp. 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: clark mp. 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.
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: clark mp. 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
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. 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
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: clark mp. 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
Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-alpha production.
Clark MP, Laughlin SK, Laufersweiler MJ, Bookland RG, Brugel TA, Golebiowski A, Sabat MP, Townes JA, VanRens JC, Djung JF, Natchus MG, De B, Hsieh LC, Xu SC, Walter RL, Mekel MJ, Heitmeyer SA, Brown KK, Juergens K, Taiwo YO, Janusz MJ. Clark MP, et al. J Med Chem. 2004 May 20;47(11):2724-7. doi: 10.1021/jm049968m. J Med Chem. 2004. PMID: 15139749
79 results