Synthesis and SAR studies of novel heteroaryl fused tetracyclic indole-diamide compounds: Potent allosteric inhibitors of the hepatitis C virus NS5B polymerase
Presented here are initial structure-activity relationship (SAR) studies on a series of novel heteroaryl fused tetracyclic indole-based inhibitors of the hepatitis C viral polymerase, NS5B. The introduction of alternative heterocyclic moieties into the indolo-fused inhibitor class significantly expands the reported SAR and resulted in the identification of pyridino analogs, typified by compounds 44 and 45 that displayed excellent potency against the NS5B polymerase of both HCV 1a and HCV 1b genotypes.
Ding, Min,He, Feng,Hudyma, Thomas W.,Zheng, Xiaofan,Poss, Michael A.,Kadow, John F.,Beno, Brett R.,Rigat, Karen L.,Wang, Ying-Kai,Fridell, Robert A.,Lemm, Julie A.,Qiu, Dike,Liu, Mengping,Voss, Stacey,Pelosi, Lenore A.,Roberts, Susan B.,Gao, Min,Knipe, Jay,Gentles, Robert G.
scheme or table
p. 2866 - 2871
(2012/05/20)
Inhibitors of HCV replication
Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.
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Page/Page column 23-24; 43
(2010/10/20)
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