Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 42, Issue 5, Pages 567-579Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2006.11.014
Keywords
NNRTT; HIV-1; diarylpyrimidine (DAPY)
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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. (c) 2006 Elsevier Masson SAS. All rights reserved.
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