Article
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
Journal of medicinal chemistry - 24 Mar 2005
Janssen Paul A J, Lewi Paul J, Arnold Eddy, Daeyaert Frits, de Jonge Marc, Heeres Jan, Koymans Luc, Vinkers Maarten, Guillemont Jérôme, Pasquier Elisabeth, Kukla Mike, Ludovici Don, Andries Koen, de Béthune Marie-Pierre, Pauwels Rudi, Das Kalyan, Clark Art D, Frenkel Yulia Volovik, Hughes Stephen H, Medaer Bart, De Knaep Fons, Bohets Hilde, De Clerck Fred, Lampo Ann, Williams Peter, Stoffels Paul
Abstract excerpt
Ideally, an anti-HIV drug should (1) be highly active against wild-type and mutant HIV without allowing breakthrough; (2) have high oral bioavailability and long elimination half-life, allowing once-daily oral treatment at low doses; (3) have minimal adverse effects; and (4) be easy to synthesize and formulate. R278474, a new diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI), appears...
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