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
  • 1. College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China. [email protected]
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.