Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 18, Pages 5482-5485Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.07.080
Keywords
Diarylpyridine derivatives; HIV-1 NNRTIs; Drug resistance
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Funding
- National Natural Science Foundation of China and Beijing government [20472114, 7052057]
- NIH [AI46221, AI33066, AI65310]
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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 EC50 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. (C) 2009 Elsevier Ltd. All rights reserved.
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