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Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties.
Zablocki JA, Elzein E, Li X, Koltun DO, Parkhill EQ, Kobayashi T, Martinez R, Corkey B, Jiang H, Perry T, Kalla R, Notte GT, Saunders O, Graupe M, Lu Y, Venkataramani C, Guerrero J, Perry J, Osier M, Strickley R, Liu G, Wang WQ, Hu L, Li XJ, El-Bizri N, Hirakawa R, Kahlig K, Xie C, Li CH, Dhalla AK, Rajamani S, Mollova N, Soohoo D, Lepist EI, Murray B, Rhodes G, Belardinelli L, Desai MC. Zablocki JA, et al. Among authors: desai mc. J Med Chem. 2016 Oct 13;59(19):9005-9017. doi: 10.1021/acs.jmedchem.6b00939. Epub 2016 Oct 3. J Med Chem. 2016. PMID: 27690427
Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study.
Mackman RL, Sangi M, Sperandio D, Parrish JP, Eisenberg E, Perron M, Hui H, Zhang L, Siegel D, Yang H, Saunders O, Boojamra C, Lee G, Samuel D, Babaoglu K, Carey A, Gilbert BE, Piedra PA, Strickley R, Iwata Q, Hayes J, Stray K, Kinkade A, Theodore D, Jordan R, Desai M, Cihlar T. Mackman RL, et al. J Med Chem. 2015 Feb 26;58(4):1630-43. doi: 10.1021/jm5017768. Epub 2015 Jan 27. J Med Chem. 2015. PMID: 25574686 Clinical Trial.
Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350).
Xu L, Liu H, Hong A, Vivian R, Murray BP, Callebaut C, Choi YC, Lee MS, Chau J, Tsai LK, Stray KM, Strickley RG, Wang J, Tong L, Swaminathan S, Rhodes GR, Desai MC. Xu L, et al. Among authors: desai mc. Bioorg Med Chem Lett. 2014 Feb 1;24(3):995-9. doi: 10.1016/j.bmcl.2013.12.057. Epub 2013 Dec 21. Bioorg Med Chem Lett. 2014. PMID: 24412072
Discovery of ledipasvir (GS-5885): a potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection.
Link JO, Taylor JG, Xu L, Mitchell M, Guo H, Liu H, Kato D, Kirschberg T, Sun J, Squires N, Parrish J, Kellar T, Yang ZY, Yang C, Matles M, Wang Y, Wang K, Cheng G, Tian Y, Mogalian E, Mondou E, Cornpropst M, Perry J, Desai MC. Link JO, et al. Among authors: desai mc. J Med Chem. 2014 Mar 13;57(5):2033-46. doi: 10.1021/jm401499g. Epub 2014 Jan 10. J Med Chem. 2014. PMID: 24320933 Clinical Trial.
Correction to Discovery of Ledipasvir (GS-5885): A Potent, Once-Daily Oral NS5A Inhibitor for the Treatment of Hepatitis C Virus Infection.
Link JO, Taylor JG, Xu L, Mitchell M, Guo H, Liu H, Kato D, Kirschberg T, Sun J, Squires N, Parrish J, Kellar T, Yang ZY, Yang C, Matles M, Wang Y, Wang K, Cheng G, Tian Y, Mogalian E, Mondou E, Cornpropst M, Perry J, Desai MC. Link JO, et al. Among authors: desai mc. J Med Chem. 2016 Aug 25;59(16):7696. doi: 10.1021/acs.jmedchem.6b01043. Epub 2016 Aug 16. J Med Chem. 2016. PMID: 27529494 No abstract available.
Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors.
Boojamra CG, Parrish JP, Sperandio D, Gao Y, Petrakovsky OV, Lee SK, Markevitch DY, Vela JE, Laflamme G, Chen JM, Ray AS, Barron AC, Sparacino ML, Desai MC, Kim CU, Cihlar T, Mackman RL. Boojamra CG, et al. Among authors: desai mc. Bioorg Med Chem. 2009 Feb 15;17(4):1739-46. doi: 10.1016/j.bmc.2008.12.028. Epub 2008 Dec 24. Bioorg Med Chem. 2009. PMID: 19179082
Discovery of GS-9131: Design, synthesis and optimization of amidate prodrugs of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148.
Mackman RL, Ray AS, Hui HC, Zhang L, Birkus G, Boojamra CG, Desai MC, Douglas JL, Gao Y, Grant D, Laflamme G, Lin KY, Markevitch DY, Mishra R, McDermott M, Pakdaman R, Petrakovsky OV, Vela JE, Cihlar T. Mackman RL, et al. Among authors: desai mc. Bioorg Med Chem. 2010 May 15;18(10):3606-17. doi: 10.1016/j.bmc.2010.03.041. Epub 2010 Mar 27. Bioorg Med Chem. 2010. PMID: 20409721
HCV versus HIV drug discovery: Déjà vu all over again?
Watkins WJ, Desai MC. Watkins WJ, et al. Among authors: desai mc. Bioorg Med Chem Lett. 2013 Apr 15;23(8):2281-7. doi: 10.1016/j.bmcl.2013.02.070. Epub 2013 Feb 26. Bioorg Med Chem Lett. 2013. PMID: 23489621 Free article. Review.
45 results