title: Anti-tubercular agents. Part 8: synthesis, antibacterial and antitubercular activity of 5-nitrofuran based 1,2,3-triazoles.
abstract: 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 μg/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 μg/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 μg/ml. These conjugates were also screened for antitubercular activity against Mycobacterium tuberculosis H37Rv strain. Compound 8e showed promising antitubercular activity with MIC value of 0.25 μg/ml. Most of these compounds are less toxic to normal mammalian cells than the widely used antibacterial drug Ciprofloxacin.
authors.affiliation: Medicinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad 500007, India. Electronic address: ahmedkamal@iict.res.in.
authors.forename: Ahmed
authors.initials: A
authors.lastname: Kamal
authors.forename: Syed Mohammed Ali
authors.initials: SM
authors.lastname: Hussaini
authors.forename: Shaikh
authors.initials: S
authors.lastname: Faazil
authors.forename: Y
authors.initials: Y
authors.lastname: Poornachandra
authors.forename: G
authors.initials: G
authors.lastname: Narender Reddy
authors.forename: C Ganesh
authors.initials: CG
authors.lastname: Kumar
authors.forename: Vikrant Singh
authors.initials: VS
authors.lastname: Rajput
authors.forename: Chitra
authors.initials: C
authors.lastname: Rani
authors.forename: Rashmi
authors.initials: R
authors.lastname: Sharma
authors.forename: Inshad Ali
authors.initials: IA
authors.lastname: Khan
authors.forename: N
authors.initials: N
authors.lastname: Jagadeesh Babu
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D018360:Crystallography, X-Ray; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D009581:Nitrofurans / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D009581:Nitrofurans; D014230:Triazoles
keywords: Antimicrobial; Antitubercular; Biofilm; MRSA; Nitrofuran; Triazole