title: Design, practical synthesis, and biological evaluation of novel 6-(pyrazolylmethyl)-4-quinoline-3-carboxylic acid derivatives as HIV-1 integrase inhibitors.
abstract: A series of novel 6-(pyrazolylmethyl)-4-oxo-4-quinoline-3-carboxylic acid derivatives bearing different substituents on the N-position of quinoline ring were designed and synthesized as potential HIV-1 integrase (IN) inhibitors, based on the structurally related GS-9137 scaffold. The structures of all new compounds were confirmed by 1H-NMR, 13C-NMR and ESI (or HRMS) spectra. Detailed synthetic protocols and the anti-IN activity studies are also presented.
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: Song
authors.initials: S
authors.lastname: Yan
authors.forename: Zaigang
authors.initials: Z
authors.lastname: Luo
authors.forename: Xiao
authors.initials: X
authors.lastname: Han
authors.forename: Yujie
authors.initials: Y
authors.lastname: Wang
authors.forename: Zhanyang
authors.initials: Z
authors.lastname: Wang
authors.forename: Chengchu
authors.initials: C
authors.lastname: Zeng
mesh_terms: D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology; D008958:Models, Molecular; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015363:Quinolones / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D002264:Carboxylic Acids; D019428:HIV Integrase Inhibitors; D011720:Pyrazoles; D011804:Quinolines; D015363:Quinolones; C509700:elvitegravir; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1