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Synthesis and Evaluation of Some Phenyl Substituted Azetidine Containing 1, 2, 4‐triazole Derivatives as Antibacterial Agents.

Authors :
Dhall, Esha
Jain, Sonika
Mishra, Achal
Dwivedi, Jaya
Sharma, Swapnil
Source :
Journal of Heterocyclic Chemistry; Dec2018, Vol. 55 Issue 12, p2859-2869, 11p
Publication Year :
2018

Abstract

A novel series of phenyl substituted azetidine containing 1, 2, 4‐triazole derivatives 7(a–j) were synthesized and characterized by IR, 1HNMR, 13CNMR, and mass spectroscopy. Synthesized 1, 2, 4‐triazole derivatives were subsequently assayed in vitro to investigate their antibacterial activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli using broth dilution method. Compounds 7c, 7d, and 7e exhibited potent inhibitory activities as compared to standard cefotaxime. Further, fluorescence spectral studies were also carried out to ascertain the antibacterial potential of compound 7c against two bacterial strains, that is, P. aeruginosa and S. aureus. In docking studies, all the compounds exhibited good docking scores between −12.04 and −11.36 kcal/mol and indicated that compounds could act through inhibition of bacterial DNA gyrase (PDB ID 3U2D). Among all, 7c has shown the maximum docking score and found in agreement to in vitro studies. In conclusion, synthesized 1, 2, 4‐triazole derivatives holds substantial caliber to be categorized as antibacterial agents. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
0022152X
Volume :
55
Issue :
12
Database :
Complementary Index
Journal :
Journal of Heterocyclic Chemistry
Publication Type :
Academic Journal
Accession number :
133557170
Full Text :
https://doi.org/10.1002/jhet.3357