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

2006; Elsevier BV; Volume: 42; Issue: 5 Linguagem: Inglês

10.1016/j.ejmech.2006.11.014

1768-3254

Céline Mordant, Benoît Schmitt, Élisabeth Pasquier, Christophe Demestre, Laurence Quéguiner, Chantal Masungi, Anik Peeters, Liesbeth Smeulders, Eva Bettens, Kurt Hertogs, Jan Heeres, Paul Lewi, Jérôme Guillemont,

Biochemical and Molecular Research

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.