title: Synthesis and biological evaluation of 5-fluoroquinolone-3-carboxylic acids as potential HIV-1 integrase inhibitors.
abstract: A series of new quinolone-3-carboxylic acids as HIV-1 integrase inhibitors featuring a fluorine atom at C-5 position were synthesized and evaluated for their antiviral activity in C8166 cell culture. These newly synthesized compounds showed anti-HIV activity against wild-type virus with an EC₅₀ value ranging from 29.85 to 0.032 μΜ. The most active compound 4e exhibited activity against wild-type virus and the mutant virus A17 with an EC₅₀ value of 0.032 and 0.082 μΜ, respectively. Preliminary structure-activity relationship of these 5-fluoroquinolone-3-carboxylic acids was also investigated.
authors.affiliation: Department of Chemistry, Fudan University, Shanghai, P R China.
authors.forename: Qiu-Qin
authors.initials: QQ
authors.lastname: He
authors.forename: Xuan
authors.initials: X
authors.lastname: Zhang
authors.forename: Liu-Meng
authors.initials: LM
authors.lastname: Yang
authors.forename: Yong-Tang
authors.initials: YT
authors.lastname: Zheng
authors.forename: Fener
authors.initials: F
authors.lastname: Chen
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D024841:Fluoroquinolones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006678:HIV / Q000187:drug effects*; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D002264:Carboxylic Acids; D024841:Fluoroquinolones; D019428:HIV Integrase Inhibitors; D019427:HIV Integrase