Design, Synthesis, Antimicrobial Evaluation of Novel 2-Oxo-4-Substituted Aryl-Azetidine Benzotriazole Derivatives

被引:3
|
作者
Rokde, Vijayshri [1 ]
Danao, Kishor [1 ]
Nimje, Juhi [1 ]
Nandurkar, Deweshri [1 ]
Yerne, Tiksha [1 ]
Yadav, Priyanka [1 ]
Mahajan, Ujwala [1 ]
机构
[1] Dadasaheb Balpande Coll Pharm, Dept Pharmaceut Chem, Nagpur 440037, Maharashtra, India
关键词
benzotriazole; azetidine; microwave; molecular docking; antimicrobial activity; INFECTIONS; PYRIMIDINE; RESISTANCE;
D O I
10.1002/cbdv.202300433
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of compounds was synthesized and characterized to explore new antimicrobial agents. These compounds were evaluated by using the agar cup plate method. The most active compound exhibited a zone of inhibition 18 & PLUSMN;0.09 mm and 19 & PLUSMN;0.09 mm against E. Coli and S. aureus, respectively. To gain insights into the intermolecular interactions, molecular docking studies were performed at the active site of the glucosamine fructose 6 phosphate synthase (GlcN 6 p) enzyme (PDB Id: 1XFF). The results of the molecular docking studies are in agreement with the pharmacological evaluation with potent compounds, exhibiting docking scores of -11.2. However, deformability, B-factor and covariance computations showed a result that the most active compound favored molecular connections with the protein. Therefore, our research is important for the development of antimicrobial agents
引用
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页数:12
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