389628-30-2Relevant academic research and scientific papers
Inhibitors of HIV-1 attachment. Part 7: Indole-7-carboxamides as potent and orally bioavailable antiviral agents
Yeung, Kap-Sun,Qiu, Zhilei,Xue, Quifen,Fang, Haiquan,Yang, Zheng,Zadjura, Lisa,D'Arienzo, Celia J.,Eggers, Betsy J.,Riccardi, Keith,Shi, Pei-Yong,Gong, Yi-Fei,Browning, Marc R.,Gao, Qi,Hansel, Steven,Santone, Kenneth,Lin, Ping-Fang,Meanwell, Nicholas A.,Kadow, John F.
supporting information, p. 198 - 202 (2013/02/25)
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.
