2. Academic Validation
  3. Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids

Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids

  • Eur J Med Chem. 2009 Mar;44(3):1205-9. doi: 10.1016/j.ejmech.2008.09.012.
Seyyedehsamira Jazayeri 1,  Mohammad Hassan Moshafi,  Loghman Firoozpour,  Saeed Emami,  Saeed Rajabalian,  Mitra Haddad,  Farahnaz Pahlavanzadeh,  Manzarbanoo Esnaashari,  Abbas Shafiee,  Alireza Foroumadi
Affiliations

Affiliation

  • 1 Department of Chemistry, Islamic Azad University, Tehran North-Branch, Tehran, Iran.
PMID: 18950903 DOI: 10.1016/j.ejmech.2008.09.012
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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