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).

@article{Janssen2005InSO,
  title={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).},
  author={Paul Adriaan Jan Janssen and Paul J. Lewi and Eddy Arnold and Frits Daeyaert and Marc R. de Jonge and Jan Heeres and Luc M. H. Koymans and Maarten H Vinkers and J{\'e}r{\^o}me Emile Georges Guillemont and Elisabeth Pasquier and Mike Kukla and Dominic A. Ludovici and Koen Andries and Marie-Pierre de B{\'e}thune and Rudi Pauwels and Kalyan Kumar Das and Art D. Clark and Yulia Volovik Frenkel and Stephen H. Hughes and Bart P. Medaer and Fons De Knaep and Hilde H Bohets and Fabrice de Clerck and Ann Lampo and Patrick Geoff Williams and Paul Stoffels},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 6},
  pages={
          1901-9
        }
}
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 to meet these criteria and to be suitable for high compliance oral treatment of HIV… CONTINUE READING
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