2. Academic Validation
  3. Design and synthesis of novel β-diketo derivatives as HIV-1 integrase inhibitors

Design and synthesis of novel β-diketo derivatives as HIV-1 integrase inhibitors

  • Bioorg Med Chem. 2012 Jan 1;20(1):177-82. doi: 10.1016/j.bmc.2011.11.014.
Liming Hu 1,  Sulei Zhang,  Xianzhuo He,  Zaigang Luo,  Xiaoli Wang,  Wei Liu,  Xuemei Qin
Affiliations

Affiliation

  • 1 College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China. huliming@bjut.edu.cn
PMID: 22154762 DOI: 10.1016/j.bmc.2011.11.014
Abstract

A series of novel β-diketo derivatives which combined the virtues of 1,3-diketo, 1,2,3-triazole and polyhydroxylated aromatics moieties, were designed and synthesized as potential HIV-1 integrase (IN) inhibitors and evaluated their inhibition to the strand transfer process of HIV-1 integrase. The result indicates that 3,4,5-trihydroxylated aromatic derivatives exhibit good inhibition to HIV-1 integrase, but dihydroxylated aromatic derivatives and corresponding methoxy aromatic derivatives appear little inhibition to HIV-1 integrase.

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