Tehran University of Medical Sciences
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
Authors: Jazayeri S , Moshafi MH , Firoozpour L , Emami S , Rajabalian S , Haddad M , Pahlavanzadeh F , Esnaashari M , Shafiee A , Foroumadi A ,
European journal of medicinal chemistry , Vol., No. 1768-3254 (Electronic) , 20090302 ,Page:0
A number of gatifloxacin analogues containing a nitroaryl-1,3,4-thiadiazole moiety attached to the piperazine ring at C-7 position were prepared and evaluated as antibacterial agents against a panel of gram-positive and gram-negative bacteria. Among synthesized compounds, nitrofuran analog 6a exhibited more potent inhibitory activity against gram-positive bacteria including Staphylococcus epidermidis (MIC=0.0078 microg/mL), Bacillus subtilis (MIC=0.0039 microg/mL), Enterococcus faecalis (MIC=0.125 microg/mL) and Micrococcus luteus (MIC=0.125 microg/mL), with respect to other synthesized compounds and reference drug gatifloxacin. The target compounds were also assessed for their cytotoxic activity against normal mouse fibroblast (NIH/3T3) cells using MTT assay. The results indicated that these compounds exhibit antibacterial activity at non-cytotoxic concentrations.