title: Design and synthesis of novel β-diketo derivatives as HIV-1 integrase inhibitors.
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.
authors.affiliation: College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China. huliming@bjut.edu.cn
authors.forename: Liming
authors.initials: L
authors.lastname: Hu
authors.forename: Sulei
authors.initials: S
authors.lastname: Zhang
authors.forename: Xianzhuo
authors.initials: X
authors.lastname: He
authors.forename: Zaigang
authors.initials: Z
authors.lastname: Luo
authors.forename: Xiaoli
authors.initials: X
authors.lastname: Wang
authors.forename: Wei
authors.initials: W
authors.lastname: Liu
authors.forename: Xuemei
authors.initials: X
authors.lastname: Qin
mesh_terms: D015195:Drug Design; D004789:Enzyme Activation / Q000187:drug effects; D019427:HIV Integrase / Q000737:chemistry* / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D007651:Keto Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry
chemical_list: D019428:HIV Integrase Inhibitors; D007651:Keto Acids; D014230:Triazoles; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1