Inhibitors of HIV-1 attachment. Part 7: indole-7-carboxamides as potent and orally bioavailable antiviral agents.

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

Bioorganic & Medicinal Chemistry Letters（2013）

Cited 51|Views14

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Abstract

Optimization of the early lead compound 1 with various carboxamide substitution at the C7 position provided heteroaryl carboxamide analogs (e.g., 35) that exhibited picomolar potency, while the simple methyl amide analog 4 displayed a promising in vitro profile and favorable pharmacokinetic properties in preclinical species.

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Key words

Antivirals,HIV-1 attachment inhibitors,Indole glyoxamide,Amides,Molecular conformation

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