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

College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China.
Bioorganic & medicinal chemistry (Impact Factor: 2.82). 11/2011; 20(1):177-82. DOI: 10.1016/j.bmc.2011.11.014
Source: PubMed

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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