title: Synthesis, characterization and biological activity of a series of carboxamide derivatives of ofloxacin.
abstract: The present study was designed to help develop new agents with better antimicrobial profiles. Specifically, we focused on modification of the basic structure of ofloxacin by introducing new functionality at its C3 position. For this purpose, the carboxylic group at the C3 position of ofloxacin was replaced by an amide group through an ester aminolysis reaction. The structure of these derivatives was established by various analytical techniques i.e., IR, (1)H-NMR, (13)C-NMR CHNS elemental analysis and mass spectrometry. The antibacterial activity of ofloxacin and its derivatives against ten different Gram-positive and Gram-negative microorganisms was studied using a disk susceptibility method. These compounds were further tested for their activity against various fungi and compared to ofloxacin. The synthesized compounds showed diverse antimicrobial profiles. Among them, a few compounds possessed a comparable or better activity in comparison to the reference drug.
authors.affiliation: Department of Chemistry, University of Karachi, Karachi 75270, Pakistan.
authors.forename: M Saeed
authors.initials: MS
authors.lastname: Arayne
authors.forename: Najma
authors.initials: N
authors.lastname: Sultana
authors.forename: Urooj
authors.initials: U
authors.lastname: Haroon
authors.forename: M Hashim
authors.initials: MH
authors.lastname: Zuberi
authors.forename: Syeda Bushra Shakeb
authors.initials: SB
authors.lastname: Rizvi
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008826:Microbial Sensitivity Tests; D015242:Ofloxacin / Q000031:analogs & derivatives* / Q000494:pharmacology; D013055:Spectrophotometry, Infrared
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D024841:Fluoroquinolones; D015242:Ofloxacin