Anti-tubercular agents. Part 8: Synthesis, antibacterial and antitubercular activity of 5-nitrofuran based 1,2,3-triazoles

作者：Kamal Ahmed^*; Hussaini Syed Mohammed Ali; Faazil Shaikh; Poornachandra Y; Reddy G Narender; Kumar C Ganesh; Rajput Vikrant Singh; Rani Chitra; Sharma Rashmi; Khan Inshad Ali; Babu N Jagadeesh

来源：Bioorganic & Medicinal Chemistry Letters, 2013, 23(24): 6842-6846.

DOI：10.1016/j.bmcl.2013.10.010

• Antimicrobial
• Antitubercular
• Nitrofuran
• Triazole
• Biofilm
• MRSA

A series of 5-nitrofuran-triazole conjugates were synthesized and evaluated for their antimicrobial activity against both Gram-positive and Gram-negative bacterial strains. All the compounds exhibited promising inhibition towards Gram-positive pathogenic strains, while mild inhibitory effects were observed towards Gram-negative bacterial strains. Some of the compounds 8a, 8b, 8e, 8f, 8h are most active among the series exhibiting MIC value of 1.17 mu g/ml against different bacterial strains. The bactericidal activity is found to be in accordance with the bacterial growth inhibition data. Compound 8e was found to be equipotent to the standard drug Ciprofloxacin displaying MBC value of 1.17 mu g/ml against the bacterial strain Bacillus subtilis. The compounds have also demonstrated promising antibacterial activity against the resistant strain MRSA and were found to be effective inhibitors of biofilm formation. The compound 8b exhibited excellent anti-biofilm activity with IC50 value as low as 0.8 mu g/ml. These conjugates were also screened for antitubercular activity against Mycobacterium tuberculosis H(37)Rv strain. Compound 8e showed promising antitubercular activity with MIC value of 0.25 mu g/ml. Most of these compounds are less toxic to normal mammalian cells than the widely used antibacterial drug Ciprofloxacin.

• 出版日期2013-12-15