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

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Mordant C,Schmitt B,Pasquier E,Demestre C,Queguiner L,Masungi C,Peeters A,Smeulders L,Bettens E,Hertogs K,Heeres J,Lewi P,Guillemont J

doi

10.1016/j.ejmech.2006.11.014

subject

Has Abstract

pub_date

2007-05-01 00:00:00

pages

567-79

issue

5

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(06)00436-3

journal_volume

42

pub_type

杂志文章

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