2. Academic Validation
  3. Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains

Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains

  • Eur J Med Chem. 2007 May;42(5):567-79. doi: 10.1016/j.ejmech.2006.11.014.
Céline Mordant 1,  Benoit Schmitt,  Elisabeth Pasquier,  Christophe Demestre,  Laurence Queguiner,  Chantal Masungi,  Anik Peeters,  Liesbeth Smeulders,  Eva Bettens,  Kurt Hertogs,  Jan Heeres,  Paul Lewi,  Jerome Guillemont
Affiliations

Affiliation

  • 1 Johnson & Johnson Pharmaceutical Research and Development, Medicinal Chemistry Department, Campus de Maigremont BP315, F-27106 Val de Reuil Cedex, France.
PMID: 17223230 DOI: 10.1016/j.ejmech.2006.11.014
Abstract

Novel diarylpyrimidines (DAPY), which represent next generation of non-nucleoside Reverse Transcriptase inhibitors (NNRTIs), were synthesized and their activities against human immunodeficiency virus type I (HIV-1) assessed. Modulations at positions 2 and 6 of the left phenyl ring generated interesting derivatives of TMC278 displaying high potency against wild-type and mutant viruses compared to nevirapine and efavirenz. The pharmacokinetic profile of the best newly synthesized DAPY was evaluated and compared with TMC278 now in phase II clinical trials.

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