| Literature DB >> 23200252 |
Kap-Sun Yeung1, Zhilei Qiu, Quifen Xue, Haiquan Fang, Zheng Yang, Lisa Zadjura, Celia J D'Arienzo, Betsy J Eggers, Keith Riccardi, Pei-Yong Shi, Yi-Fei Gong, Marc R Browning, Qi Gao, Steven Hansel, Kenneth Santone, Ping-Fang Lin, Nicholas A Meanwell, John F Kadow.
Abstract
A series of substituted carboxamides at the indole C7 position of the previously described 4-fluoro-substituted indole HIV-1 attachment inhibitor 1 was synthesized and the SAR delineated. Heteroaryl carboxamide inhibitors that exhibited pM potency in the primary cell-based assay against a pseudotype virus expressing a JRFL envelope were identified. The simple methyl amide analog 4 displayed a promising in vitro profile, with its favorable HLM stability and membrane permeability translating into favorable pharmacokinetic properties in preclinical species.Entities:
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Year: 2012 PMID： 23200252 DOI： 10.1016/j.bmcl.2012.10.115
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823