Evaluation of antimycobacterial and DNA gyrase inhibition of fluoroquinolone derivatives

The Journal of General and Applied Microbiology

Tanushree Ratan Bal¹  Valakunja Nagaraja²  Deshpande R. Radha²  Dharmarajan Sriram¹  Perumal Yogeeswari¹ 

[1] Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science;Department of Microbiology and Cell Biology, Indian Institute of Science

关键词: DNA gyrase inhibition;    fluoroquinolone derivatives;    isatin derivatives;    Mycobacterium smegmatis;    Mycobacterium tuberculosis;   

DOI  :  10.2323/jgam.52.195

学科分类：微生物学和免疫学

来源: Applied Microbiology, Molecular and Cellulrar Biosciences Research Foundation

【 摘 要 】

The antimycobacterial activity (both in vitro and in vivo) and DNA gyrase inhibition of newly synthesized fluoroquinolone derivatives were tested against Mycobacterium tuberculosis H37Rv and Mycobacterium smegmatis, respectively. Among the synthesized compounds, compound F11 was found to exhibit the most potent in vitro antimycobacterial activity with a MIC value of 0.78 μg/ml, and a selectivity index of more than 80 while not being cytotoxic to the Vero cell line up to 62.5 μg/ml. When evaluated for in vivo antimycobacterial activity, compound F11 demonstrated a paramount decrease of bacterial load in lung and spleen tissues compared to the control and better than the standard drug ciprofloxacin.

【 授权许可】

Unknown