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Synthesis and evaluation against hepatitis C virus of 7-deaza analogues of 2'-C-methyl-6-O-methyl guanosine nucleoside and L-Alanine ester phosphoramidates.
Bourdin C, McGuigan C, Brancale A, Chamberlain S, Vernachio J, Hutchins J, Gorovits E, Kolykhalov A, Muhammad J, Patti J, Henson G, Bleiman B, Bryant KD, Ganguly B, Hunley D, Obikhod A, Walters CR, Wang J, Ramamurty CV, Battina SK, Srivinas Rao C. Bourdin C, et al. Among authors: bleiman b. Bioorg Med Chem Lett. 2013 Apr 1;23(7):2260-4. doi: 10.1016/j.bmcl.2012.12.004. Epub 2012 Dec 20. Bioorg Med Chem Lett. 2013. PMID: 23453067
Phosphorodiamidates as a promising new phosphate prodrug motif for antiviral drug discovery: application to anti-HCV agents.
McGuigan C, Madela K, Aljarah M, Bourdin C, Arrica M, Barrett E, Jones S, Kolykhalov A, Bleiman B, Bryant KD, Ganguly B, Gorovits E, Henson G, Hunley D, Hutchins J, Muhammad J, Obikhod A, Patti J, Walters CR, Wang J, Vernachio J, Ramamurty CV, Battina SK, Chamberlain S. McGuigan C, et al. Among authors: bleiman b. J Med Chem. 2011 Dec 22;54(24):8632-45. doi: 10.1021/jm2011673. Epub 2011 Nov 16. J Med Chem. 2011. PMID: 22039920
INX-08189, a phosphoramidate prodrug of 6-O-methyl-2'-C-methyl guanosine, is a potent inhibitor of hepatitis C virus replication with excellent pharmacokinetic and pharmacodynamic properties.
Vernachio JH, Bleiman B, Bryant KD, Chamberlain S, Hunley D, Hutchins J, Ames B, Gorovits E, Ganguly B, Hall A, Kolykhalov A, Liu Y, Muhammad J, Raja N, Walters CR, Wang J, Williams K, Patti JM, Henson G, Madela K, Aljarah M, Gilles A, McGuigan C. Vernachio JH, et al. Among authors: bleiman b. Antimicrob Agents Chemother. 2011 May;55(5):1843-51. doi: 10.1128/AAC.01335-10. Epub 2011 Feb 28. Antimicrob Agents Chemother. 2011. PMID: 21357300 Free PMC article.