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

Novel thiazolidine-2,4-dione carboxamide and amino acid derivatives were synthesized in excellent yield using OxymaPure/<i>N,N&#8242;</i>-diisopropylcarbodimide coupling methodology and were characterized by chromatographic and spectrometric methods, and elemental analysis. The antim...

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Bibliographic Details
Main Authors: Rakia Abd Alhameed, Zainab Almarhoon, Sarah I. Bukhari, Ayman El-Faham, Beatriz G. de la Torre, Fernando Albericio
Format: Article
Language:English
Published: MDPI AG 2019-12-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/25/1/105
Description
Summary:Novel thiazolidine-2,4-dione carboxamide and amino acid derivatives were synthesized in excellent yield using OxymaPure/<i>N,N&#8242;</i>-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 (<i>Staphylococcus aureus</i> and <i>Bacillus subtilis</i>), two-Gram negative bacteria (<i>Escherichia coli</i> and <i>Pseudomonas aeruginosa</i>), and one fungal isolate (<i>Candida albicans).</i> 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 <i>S. aureus</i>.
ISSN:1420-3049