Synthesis and antibacterial, antimycobacterial and docking studies of novel N-piperazinyl fluoroquinolones

被引:18
作者
Agrawal, Kapil M. [1 ]
Talele, Gokul S. [2 ]
机构
[1] RC Patel Inst Pharmaceut Educ & Res, Dept Pharmaceut Chem, Dhule 425405, Maharashtra, India
[2] Nasik Gramin Shikshan Prasarak Mandal Coll Pharm, Dept Pharmaceut Chem, Nasik 422213, Maharashtra, India
关键词
Fluoroquinolone (FQ); Antibacterial; Antimycobacterial; Cytotoxicity; Docking study; MULTIDRUG-RESISTANT TUBERCULOSIS; SHORT-COURSE CHEMOTHERAPY; PULMONARY TUBERCULOSIS; MYCOBACTERIUM-TUBERCULOSIS; PHASE-II; DERIVATIVES; MOXIFLOXACIN; OFLOXACIN; AGENTS; OUTCOMES;
D O I
10.1007/s00044-012-0074-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The present study deals with the synthesis of some novel fluoroquinolone derivatives as antibacterial and antitubercular agents. The titled compounds 7a-g and 8a-g were found to possess comparable or more potent activity than the reference compounds ciprofloxacin, norfloxacin, isoniazid and rifampicin. The synthesized compounds showed activity against S. aureus and C. bacterium, whereas poor activity was observed against P. aeruginosa and E. coli. These compounds were subjected to in vitro cytotoxicity study by MTT assay, and their selectivity index was calculated. Compound 7d was found to be the most efficient antimycobacterial agent amongst the series. Molecular docking revealed that synthesized derivatives and target proteins were actively involved in a binding pattern and had significant correlation with biological activity. Novel N-piperazinyl fluoroquinolone derivatives were synthesized and evaluated for their in vitro antibacterial, antimycobacterial and cytotoxic properties. Activity results were compared with the docking results.
引用
收藏
页码:818 / 831
页数:14
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