Synthesis, Molecular Docking of New N-(2-(4-(1h-Pyrrol-1-yl)Phenoxy)-N′-2-(Substituted Phenoxy)Acetyl)Acetohydrazides Derivatives as Antibacterial and Antitubercular Analogs

被引:0
|
作者
Alqahtani, Yahya S. [1 ]
Kumar, Prem S. R. [2 ]
Veerkumar [2 ]
Shaikh, Ibrahim Ahmed [3 ]
Joshi, Shrinivas D. [2 ]
机构
[1] Najran Univ, Coll Pharm, Dept Pharmaceut Chem, Najran 66462, Saudi Arabia
[2] Soniya Educ Trusts Coll Pharm, Dept Pharmaceut Chem, Novel Drug Design & Discovery Lab, Dharwad 580002, Karnataka, India
[3] Najran Univ, Coll Pharm, Dept Pharmacol, Najran 66462, Saudi Arabia
关键词
Pyrrolyl-acetohydrzides; In-silico Molecular docking; Mycobacterium tuberculosis H(37)Rv; Antibacterial activity; PROTEIN-LIGAND INTERACTIONS; MYCOBACTERIUM-TUBERCULOSIS; PHTHALAZINONE; VALIDATION; BM212;
D O I
暂无
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Newer series of N-(2-(4-(1H-pyrrol-1-yl)phenoxy)-N'-(2-(substituted phenoxy) acetyl)acetohydrazides 6(a-k) was prepared by the reaction of 2-(4-(1H-pyrrol-1-yl)phenoxy) acetohydrazide (4) and substituted phenoxy acids 5(a-k) in distilled N',N'-dimethyl formamide using coupling agent 2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate and N',N'-diisopropylethylamine as a catalytic agent. The newly described compounds showed same kind of binding interface at the active site of the enzyme as that of ligand moiety. All 11 stated molecules were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis H(37)Rv strain and antibacterial activity against Gram +ve Staphylococcus aureus and Gram-ve Escherichia coli strain, all the tested molecules have shown prominent inhibitory concentration values towards both tubercular and bacterial strains.
引用
收藏
页码:159 / 167
页数:9
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