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In search of a novel anti-HIV drug: Multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6dimethylphenyl] amino]-2-pyrimidinyl]amino]-benzonitrile (R278474, rilpivirine)

  1. Author:
    Janssen, P. A. J.
    Lewi, P. J.
    Arnold, E.
    Daeyaert, F.
    de Jonge, M.
    Heeres, J.
    Koymans, L.
    Vinkers, M.
    Guillemont, J.
    Pasquier, E.
    Kukla, M.
    Ludovici, D.
    Andries, K.
    de Bethune, M. P.
    Pauwels, R.
    Das, K.
    Clark, A. D.
    Frenkel, Y. V.
    Hughes, S. H.
    Medaer, B.
    De Knaep, F.
    Bohets, H.
    De Clerck, F.
    Lampo, A.
    Williams, P.
    Stoffels, P.

  2. Author Address

    Janssen Pharmaceut, B-2350 Vosselaar, Belgium. Rutgers State Univ, Ctr Adv Biotechnol & Med, Piscataway, NJ 08854 USA. Rutgers State Univ, Dept Chem & Chem Biol, Piscataway, NJ 08854 USA. Johnson & Johnson Pharmaceut Res & Dev, Med Chem, Janssen Cilag France, F-27106 Val De Reuil, France. Johnson & Johnson Pharmaceut Res & Dev, Drug Discovery, Spring House, PA 19477 USA. Tibotec, B-2800 Mechelen, Belgium. NCI, Frederick, MD 21702 USA. Johnson & Johnson Pharmaceut Res & Dev, Drug Evaluat, B-2340 Beerse, Belgium. Johnson & Johnson Pharmaceut Res & Dev, Drug Dev, B-2340 Beerse, Belgium. Johnson & Johnson Pharmaceut Res & Dev, Drug Evaluat, High Wycombe HP144GT, Bucks, England Lewi, PJ, Janssen Pharmaceut, B-2350 Vosselaar, Belgium
    1. Year: 2005
    2. Date: MAR 24
  2. Journal: Journal of Medicinal Chemistry
    1. 48
    2. 6
    3. Pages: 1901-1909
  4. Type of Article: Article
  1. Abstract:

    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-1 infection. The discovery of R278474 was the result of a coordinated multidisciplinary effort involving medicinal chemists, virologists, crystallographers, molecular modelers, toxicologists, analytical chemists, pharmacists, and many others

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External Sources

  1. View record in Web of Science®
  2. WOS: 000227749300027

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