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Inhibitors of HIV-1 attachment. Part 7: Indole-7-carboxamides as potent and orally bioavailable antiviral agents |
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| Authors: | Kap-Sun Yeung 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 |
| Affiliation: | Bristol-Myers Squibb Research & Development, 5 Research Parkway, PO Box 5100, Wallingford, CT 06492, USA |
| 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. |
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