Evaluation of antimycobacterial and DNA gyrase inhibition of fluoroquinolone derivatives.
The antimycobacterial activity (both in vitro and in vivo) and DNA gyrase inhibition of newly synthesized fluoroquinolone derivatives were tested against Mycobacterium tuberculosis H(37)Rv 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 microg/ml, and a selectivity index of more than 80 while not being cytotoxic to the Vero cell line up to 62.5 microg/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.
Sriram
Dharmarajan
D
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani, India. dsiram@bits-pilani.ac.in
Bal
Tanushree Ratan
TR
Yogeeswari
Perumal
P
Radha
Deshpande R
DR
Nagaraja
Valakunja
V
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D024841:Fluoroquinolones / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D020102:Mycobacterium smegmatis / Q000187:drug effects*; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D059005:Topoisomerase II Inhibitors; D014709:Vero Cells
D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D059005:Topoisomerase II Inhibitors