Mannich bases of 7-piperazinylquinolones and kojic acid derivatives: Synthesis, in?vitro antibacterial activity and in silico study
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- 作者：Saeed Emami ; Ebrahim Ghafouri ; Mohammad Ali Faramarzi ; Nasrin Samadi ; Hamid Irannejad ; Alireza Foroumadi
- 关键词：Antibacterial activity ; Quinolones ; Kojic acid ; Mannich bases ; Docking study
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2013
- 出版时间：October, 2013
- 年：2013
- 卷：68
- 期：Complete
- 页码：185-191
- 全文大小：792 K
文摘
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 ¡Ü0.19?¦Ìg/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.