Synthesis and biological evaluation of newer 1,3,4-oxadiazoles incorporated with benzothiazepine and benzodiazepine moieties

Patel Navin, Patel Sarvil, Purohit Amit, Patel Divyesh, Rajani Dhansukh, Rosa Moo-Puc, Gildardo Rivera

Research output: Contribution to journalArticlepeer-review

12 Scopus citations

Abstract

A series of thiazepines and diazepines having 1,3,4-oxadiazole moiety were synthesized, and they were analyzed for their in vitro antimicrobial activity against several bacteria (Staphylococcus aureus, Staphylococcus pyogenes, Escherichia coli, and Pseudomonas aeruginosa) and fungi (Candida albicans, Aspergillus Niger, and Aspergillus Clavatus) and protozoa (Entamoeba histolytica, Giardia lamblia, Trypanosoma cruzi and Leishmania mexicana). Few of the selected compounds were tested for their antitubercular activity. However, it was noticed that the potency of final analogs against each strain placed reliance on the type of substituent present on aryl ring of oxadiazole as well as presence of thiophene, pyridine, and furan at benzothiazepines and benzodiazepines. The biological screening identified that some of the compounds were found to possess good antimicrobial and antitubercular (62.5-100 μg/mL of MIC) activity.

Original languageEnglish
Pages (from-to)133-146
Number of pages14
JournalZeitschrift fur Naturforschung - Section C Journal of Biosciences
Volume72
Issue number3-4
DOIs
StatePublished - 1 Mar 2017

Keywords

  • 1,3,4-Oxadiazole
  • antimicrobial activity
  • antituberculosis activity
  • benzodiazepines
  • benzothiazepines

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