Abstract
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
Mini-Reviews in Medicinal Chemistry
Title: Sulfanyltriazole/tetrazoles: A Promising Class of HIV-1 NNRTIs
Volume: 9 Issue: 8
Author(s): Peng Zhan, Zhenyu Li, Xinyong Liu and Erik De Clercq
Affiliation:
Keywords: AIDS, HIV-1, reverse transcriptase (RT), sulfanyltriazole/tetrazoles, NNRTIs, SAR, scaffold hopping
Abstract: 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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Cite this article as:
Zhan Peng, Li Zhenyu, Liu Xinyong and De Clercq Erik, Sulfanyltriazole/tetrazoles: A Promising Class of HIV-1 NNRTIs, Mini-Reviews in Medicinal Chemistry 2009; 9 (8) . https://dx.doi.org/10.2174/138955709788681618
DOI https://dx.doi.org/10.2174/138955709788681618 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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