Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

作者：Tian Xingtao; Qin Bingjie; Lu Hong; Lai Weihong; Jiang Shibo; Lee Kuo Hsiung; Chen Chin Ho; Xie Lan^*

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(18): 5482-5485.

DOI：10.1016/j.bmcl.2009.07.080

• Diarylpyridine derivatives
• HIV-1 NNRTIs
• Drug resistance

Two series (4 and 5) of diarylpyridine derivatives were designed, synthesized, and evaluated for anti-HIV-1 activity. The most promising compound, 5e, inhibited HIV-1 IIIB, NL4-3, and RTMDR1 with low nanomolar EC(50) values and selectivity indexes of >10,000. The results of this study indicate that diarylpyridine can be used as a novel scaffold to derive a new class of potent NNRTIs, active against both wild-type and drug-resistant HIV-1 strains.

• 出版日期2009-9-15