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Bioorg Med Chem Lett. 2012 Apr 1;22(7):2376-9. doi: 10.1016/j.bmcl.2012.02.055. Epub 2012 Feb 24.

Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.

Author information

1
Beijing Institute of Pharmacology & Toxicology, 27 Tai-Ping Road, Beijing 100850, China.

Abstract

The current optimization of 2,4-diarylaniline analogs (DAANs) on the central phenyl ring provided a series of new active DAAN derivatives 9a-9e, indicating an accessible modification approach that could improve anti-HIV potency against wild-type and resistant strains, aqueous solubility, and metabolic stability. A new compound 9e not only exhibited extremely high potency against wild-type virus (EC(50) 0.53 nM) and several resistant viral strains (EC(50) 0.36-3.9 nM), but also showed desirable aqueous solubility and metabolic stability, which were comparable or better than those of the anti-HIV-1 drug TMC278 (2). Thus, new compound 9e might be a potential drug candidate for further development of novel next-generation NNRTIs.

PMID:
22406117
PMCID:
PMC3309038
DOI:
10.1016/j.bmcl.2012.02.055
[Indexed for MEDLINE]
Free PMC Article

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