title: Synthesis and biological evaluation of a class of quinolone triazoles as potential antimicrobial agents and their interactions with calf thymus DNA.
abstract: A novel series of quinolone triazoles were synthesized and characterized by IR, NMR, MS and HRMS spectra. All the newly prepared compounds were screened for their antimicrobial activities against seven bacteria and four fungi. Bioactive assay manifested that most of new compounds exhibited good or even stronger antibacterial and antifungal activities against the tested strains including multi-drug resistant MRSA in comparison with reference drugs Norfloxacin, Chloromycin and Fluconazole. The preliminary interactive investigations of compound 6b with calf thymus DNA by fluorescence and UV-vis spectroscopic methods revealed that compound 6b could effectively intercalate DNA to form compound 6b-DNA complex which might block DNA replication and thus exert its antimicrobial activities.
authors.affiliation: Laboratory of Bioorganic & Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, PR China.
authors.forename: Sheng-Feng
authors.initials: SF
authors.lastname: Cui
authors.forename: Yu
authors.initials: Y
authors.lastname: Ren
authors.forename: Shao-Lin
authors.initials: SL
authors.lastname: Zhang
authors.forename: Xin-Mei
authors.initials: XM
authors.lastname: Peng
authors.forename: Guri L V
authors.initials: GL
authors.lastname: Damu
authors.forename: Rong-Xia
authors.initials: RX
authors.lastname: Geng
authors.forename: Cheng-He
authors.initials: CH
authors.lastname: Zhou
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D002417:Cattle; D004247:DNA / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism*; D004261:DNA Replication / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D005658:Fungi / Q000187:drug effects; D007364:Intercalating Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D013056:Spectrophotometry, Ultraviolet; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000890:Anti-Infective Agents; D007364:Intercalating Agents; D015363:Quinolones; D014230:Triazoles; D004247:DNA; C427203:calf thymus DNA