title: Mannich bases of 7-piperazinylquinolones and kojic acid derivatives: synthesis, in vitro antibacterial activity and in silico study.
abstract: Novel Mannich bases of 7-piperazinylquinolones with kojic acid and chlorokojic acid were designed as new quinolone antibacterials. All compounds showed significant in vitro antibacterial activity against both Gram-positive and Gram-negative bacteria. Particularly, chlorokojic derivative 2b was the most potent compound against Staphylococcus aureus and Pseudomonas aeruginosa (MIC values≤0.19 μg/mL). Its activity was 4-8 times more than that of standard drug norfloxacin. The molecular docking study of compound 2b further supported the molecular basis of the designed compounds.
authors: Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran. Electronic address: sd_emami@yahoo.com.
authors: Saeed
authors: S
authors: Emami
authors: Ebrahim
authors: E
authors: Ghafouri
authors: Mohammad Ali
authors: MA
authors: Faramarzi
authors: Nasrin
authors: N
authors: Samadi
authors: Hamid
authors: H
authors: Irannejad
authors: Alireza
authors: A
authors: Foroumadi
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008352:Mannich Bases / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D009643:Norfloxacin / Q000737:chemistry / Q000494:pharmacology; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011753:Pyrones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D008352:Mannich Bases; D010879:Piperazines; D011753:Pyrones; D015363:Quinolones; C011890:kojic acid; D009643:Norfloxacin
keywords: Antibacterial activity; Docking study; Kojic acid; Mannich bases; Quinolones