Bioorganic and Medicinal Chemistry Letters p. 2866 - 2871 (2012)
Update date:2022-08-03
Topics:
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.
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.
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