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

C Mordant, B Schmitt, E Pasquier, C Demestre…

Index: Mordant, Celine; Schmitt, Benoit; Pasquier, Elisabeth; Demestre, Christophe; Queguiner, Laurence; Masungi, Chantal; Peeters, Anik; Smeulders, Liesbeth; Bettens, Eva; Hertogs, Kurt; Heeres, Jan; Lewi, Paul; Guillemont, Jerome European Journal of Medicinal Chemistry, 2007 , vol. 42, # 5 p. 567 - 579

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Citation Number: 58

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 ...