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

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

  • Bioorg Med Chem Lett. 2006 Aug 15;16(16):4174-7. doi: 10.1016/j.bmcl.2006.05.096.
Zhiwei Wang 1,  Baogen Wu,  Kelli L Kuhen,  Badry Bursulaya,  Truc N Nguyen,  Deborah G Nguyen,  Yun He
Affiliations

Affiliation

  • 1 Genomics Institute of the Novartis Research Foundation (GNF), San Diego, CA 92121, USA.
PMID: 16781149 DOI: 10.1016/j.bmcl.2006.05.096
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.

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