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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Sulfanyltriazole/tetrazoles: A Promising Class of HIV-1 NNRTIs

Author(s): Peng Zhan, Zhenyu Li, Xinyong Liu and Erik De Clercq

Volume 9, Issue 8, 2009

Page: [1014 - 1023] Pages: 10

DOI: 10.2174/138955709788681618

Price: $65


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.

Keywords: AIDS, HIV-1, reverse transcriptase (RT), sulfanyltriazole/tetrazoles, NNRTIs, SAR, scaffold hopping

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