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Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.

Wang, Zhiwei and Wu, Baogen and Kuhen, Kelli and Bursulaya, Badry and Nguyen, Truc and Nguyen, Deborah and He, Yun (2006) Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. Bioorganic & Medicinal Chemistry Letters, 16 (16). pp. 4174-4177. ISSN 0960-894X

Abstract

A novel sulfanyltriazole was discovered as an HIV-1 non-nucleoside reverse transcriptase inhibitor via HTS using a cell-based assay. Chemical modifications and molecular modeling studies were carried out to establish its SAR and understand its interactions with the enzyme. These modifications led to the identification of sulfanyltriazoles with low nanomolar potency for inhibiting HIV-1 replication and promising activities against selected NNRTI resistant mutants. These novel and potent sulfanyltriazoles could serve as advanced leads for further optimization.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Sulfanyltriazoles; HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI); SAR; Molecule modeling; HIV replication
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Date Deposited: 14 Dec 2009 14:04
Last Modified: 31 Jan 2013 01:26
URI: https://oak.novartis.com/id/eprint/147

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