Article
Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
Bioorganic & medicinal chemistry letters - 15 Jun 2017
Wei Lei, Wang Hui-Ling, Huang Li, Chen Chin-Ho, Morris-Natschke Susan L, Lee Kuo-Hsiung, Xie Lan
Abstract excerpt
On the basis of our prior structure-activity relationship (SAR) results, our current lead optimization of 1,5-diarylanilines (DAANs) focused on the 4-substituent (R1) on the central phenyl ring as a modifiable position related simultaneously to improved drug resistance profiles and drug-like properties. Newly synthesized p-cyanovinyl-DAANs (8a-8g) with different R1 side chains plus prior active p-cyanoethyl-DAANs...
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