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微波辅助杂环二羧酸作为潜在的抗真菌和抗菌药物

Microwave-assisted Heterocyclic Dicarboxylic Acids as Potential Antifungal and Antibacterial Drugs.

作者信息

Dabholkar V V, Parab S D

机构信息

Organic Research Laboratory, Department of Chemistry, Kishinchand Chellaram College, D. W. Road, Churchgate, Mumbai-400 020, India.

出版信息

Indian J Pharm Sci. 2011 Mar;73(2):199-207. doi: 10.4103/0250-474x.91581.

Abstract

A series of new dicarboxylic acid derivatives of 1,3,4-thiadiazines, 1,4-benzopiperizines, 1,4-thiazines, 1,3-thiazoles, 1,3-oxazoles and 1,3-imidazoles have been synthesized in 80-87% yield by the environmentally benign microwave induced technique involving the cyclocondensation of 2,3-dibromosuccinic acid with 2-aminothiophenol, o-phenylene diamine, 1,2,4-triazole, amidinothiocarbamide, amidinocarbamide and guanidine hydrochloride. The structures of all newly synthesized compounds have been established on the basis of analytical and spectral data. Evaluation of antibacterial and antifungal activity showed that almost all compounds exhibited better results than reference drugs thus they could be promising candidates for novel drugs.

摘要

通过环境友好的微波诱导技术,以2,3-二溴琥珀酸与2-氨基苯硫酚、邻苯二胺、1,2,4-三唑、氨基硫脲、氨基脲和盐酸胍进行环缩合反应,合成了一系列新的1,3,4-噻二嗪、1,4-苯并哌嗪、1,4-噻嗪、1,3-噻唑、1,3-恶唑和1,3-咪唑二羧酸衍生物,产率为80-87%。所有新合成化合物的结构均基于分析和光谱数据确定。抗菌和抗真菌活性评估表明,几乎所有化合物的效果均优于参考药物,因此它们可能是新型药物的有前途的候选者。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab21/3267305/fd0513575b4b/IJPhS-73-199-g001.jpg

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