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  • Title: Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
    Author: Jazayeri S, Moshafi MH, Firoozpour L, Emami S, Rajabalian S, Haddad M, Pahlavanzadeh F, Esnaashari M, Shafiee A, Foroumadi A.
    Journal: Eur J Med Chem; 2009 Mar; 44(3):1205-9. PubMed ID: 18950903.
    Abstract:
    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.
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