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新型噻唑烷-2,4-二酮羧酸酰胺和氨基酸衍生物的合成及抑菌活性。

Synthesis and Antimicrobial Activity of a New Series of Thiazolidine-2,4-diones Carboxamide and Amino Acid Derivatives.

机构信息

Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.

Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 4584, Riyadh 11451, Saudi Arabia.

出版信息

Molecules. 2019 Dec 27;25(1):105. doi: 10.3390/molecules25010105.

Abstract

Novel thiazolidine-2,4-dione carboxamide and amino acid derivatives were synthesized in excellent yield using OxymaPure/-diisopropylcarbodimide coupling methodology and were characterized by chromatographic and spectrometric methods, and elemental analysis. The antimicrobial and antifungal activity of these derivatives was evaluated against two Gram-positive bacteria ( and ), two-Gram negative bacteria ( and ), and one fungal isolate ( Interestingly, several samples demonstrated weak to moderate antibacterial activity against Gram-negative bacteria, as well as antifungal activity. However, only one compound namely, 2-(5-(3-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl)acetic acid, showed antibacterial activity against Gram-positive bacteria, particularly .

摘要

新型噻唑烷-2,4-二酮羧酰胺和氨基酸衍生物采用 OxymaPure/-二异丙基碳二亚胺偶联方法高产率合成,并通过色谱和光谱方法以及元素分析进行了表征。这些衍生物的抗菌和抗真菌活性针对两种革兰氏阳性菌( 和 )、两种革兰氏阴性菌( 和 )和一种真菌分离株( )进行了评估。有趣的是,一些样品对革兰氏阴性菌表现出弱至中等的抗菌活性,以及抗真菌活性。然而,只有一种化合物,即 2-(5-(3-甲氧基亚苄基)-2,4-二氧代噻唑烷-3-基)乙酸,对革兰氏阳性菌,特别是 ,表现出抗菌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/029b/6983134/0e93c376eabc/molecules-25-00105-g001.jpg

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