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合成氨苄西林和阿莫西林的2-氧代喹啉-3-甲酰胺作为铜绿假单胞菌青霉素结合蛋白1A的抑制剂

Synthesis of 2-oxoquinoline-3-carboxamide of ampicillin and amoxicillin as inhibitors of penicillin binding protein 1A of pseudomonas aeruginosa.

作者信息

Shelke Jayant, Meshram Gangadhar, Dongre Prabhkar

机构信息

Department of Chemistry, Department of Biophysics, University of Mumbai, Vidynagari, Kalina, Santacruz (East), Mumbai 400 098, India.

出版信息

Acta Pol Pharm. 2012 Jul-Aug;69(4):623-8.

PMID:22876604
Abstract

A series of ampicillin and amoxicillin derivatives were prepared by N-acylation with N1-substituted 1, 2-dihydro-2-oxoquinoline carboxylic acids by Schotten-Baumann procedure and evaluated as inhibitors of Pseudomonas aeruginosa using molecular docking study. Most of the derivatives showed remarkableactivity against Gram positive and Gram negative bacteria in vitro.

摘要

通过肖滕-鲍曼反应，用N1-取代的1,2-二氢-2-氧代喹啉羧酸进行N-酰化反应制备了一系列氨苄青霉素和阿莫西林衍生物，并使用分子对接研究评估其作为铜绿假单胞菌抑制剂的活性。大多数衍生物在体外对革兰氏阳性菌和革兰氏阴性菌显示出显著活性。

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