| Literature DB >> 17223230 |
Céline Mordant1, Benoit Schmitt, Elisabeth Pasquier, Christophe Demestre, Laurence Queguiner, Chantal Masungi, Anik Peeters, Liesbeth Smeulders, Eva Bettens, Kurt Hertogs, Jan Heeres, Paul Lewi, Jerome Guillemont.
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.Entities:
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Year: 2006 PMID： 17223230 DOI： 10.1016/j.ejmech.2006.11.014
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514