Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 17, Issue 17, Pages 6374-6379Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.07.027
Keywords
HIV-1; AIDS; NNRTIs; Selenadiazole; Anti-HIV-1 activity
Funding
- National Natural Science Foundation of China (NSFC) [30371686, 30772629, 30873133]
- International Cooperation, Ministry of Science and Technology of China [2003DF000033]
- Doctoral Program of Higher Education of China [070422083]
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The development of new HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating novel structures of increased potency. Based on the bioisosteric principle, novel series of 1,2,3-selenadiazole thioacetanilide derivatives were designed, and synthesized using an original synthetic route, structurally confirmed by spectral analysis, and evaluated for their anti-HIV activity in MT-4 cells. The results showed that only compound 7f possessed potent activity against HIV-1 replication (EC50 = 2.45 mu M) similar to the prototype series of sulfanyltriazoles. None of the compounds were active against HIV-2 replication. Crown Copyright (C) 2009 Published by Elsevier Ltd. All rights reserved.
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