Synthesis and SAR studies of novel heteroaryl fused tetracyclic indole-diamide compounds: Potent allosteric inhibitors of the hepatitis C virus NS5B polymerase

详细信息	查看全文 | 推荐本文 |

• 作者：Min Ding^a ; ^{min.ding@bms.com} ; Feng He^a ; Thomas W. Hudyma^a ; Xiaofan Zheng^a ; Michael A. Poss^a ; John F. Kadow^c ; Brett R. Beno^a ; Karen L. Rigat^b ; Ying-Kai Wang^b ; Robert A. Fridell^b ; Julie A. Lemm^b ; Dike Qiu^b ; Mengping Liu^b ; Stacey Voss^b ; Lenore A. Pelosi^b ; Susan B. Roberts^b ; Min Gao^b ; Jay Knipe^a ; Robert G. Gentles^a
• 关键词：HCV NS5B polymerase inhibitors ; Tetracyclic indoles
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 April, 2012
• 卷：22
• 期：8
• 页码：2866-2871
• 文件大小：873 K

摘要

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.