Journal
MINI-REVIEWS IN MEDICINAL CHEMISTRY
Volume 9, Issue 8, Pages 1014-1023Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/138955709788681618
Keywords
AIDS; HIV-1; reverse transcriptase (RT); sulfanyltriazole/tetrazoles; NNRTIs; SAR; scaffold hopping
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Funding
- National Natural Science Foundation of China [30873133, 30772629, 30371686]
- Key Project of The International Cooperation
- Ministry of Science and Technology of China [2003DF000033]
- Research Fund for the Doctoral Program of Higher Education of China [070422083]
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There is an urgent need for the design and development of new and safer drugs for the treatment of human immunodeficiency virus (HIV) infection, specifically active against drug-resistant viral strains. Recently, sulfanyltriazole/tetrazole derivatives were reported as potent HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs), with low nanomolar intrinsic activity against RT and submicromolar antiviral activity in HIV infected cells. In this review, the structural modifications, SAR analysis and docking studies of sulfanyltriazole/tetrazoles HIV-1 NNRTIs are discussed, and other interesting NNRTIs with the same or similar pharmacophore as the sulfanyltriazole/tetrazole derivatives are also presented and analyzed for their in SAR.
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