2. Academic Validation
  3. Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro

Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro

  • Bioorg Med Chem Lett. 2007 Aug 15;17(16):4476-80. doi: 10.1016/j.bmcl.2007.06.008.
Pi Cheng 1,  Zhi-Yong Jiang,  Rui-Rui Wang,  Xue-Mei Zhang,  Qian Wang,  Yong-Tang Zheng,  Jun Zhou,  Ji-Jun Chen
Affiliations

Affiliation

  • 1 State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, The Chinese Academy of Sciences, Kunming, Yunnan 650204, PR China.
PMID: 17574419 DOI: 10.1016/j.bmcl.2007.06.008
Abstract

A variety of N-acetyl-beta-aryl-1,2-didehydroethylamines were synthesized by direct reduction-acetylation of beta-aryl-nitroolefins and assayed as HIV-1 non-nucleoside Reverse Transcriptase inhibitors (NNRTIs) for the first time. Compound 7a exhibited a TI value of >13.2 with CC50 value of >0.787 mM in C8166 cells. This structure-activity relationship (SAR) study provided a new lead for design and discovery of more potent and selective analogues act as NNRTIs.

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