Novel arylhydrazone derivatives bearing a rhodanine moiety: synthesis and evaluation of their antibacterial activities

• Published in: Archives of pharmacal research Vol. 37; no. 7; pp. 852 - 861
• Main Authors: Li, Wei, Zheng, Chang-Ji, Sun, Liang-Peng, Song, Ming-Xia, Wu, Yan, Li, Yin-Jing, Liu, Yi, Piao, Hu-Ri
• Format: Journal Article
• Language: English
• Published: Heidelberg Pharmaceutical Society of Korea 01.07.2014; 대한약학회
• Subjects: Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - pharmacology; Drug Evaluation, Preclinical - methods; HeLa Cells; Humans; Hydrazones - chemical synthesis; Hydrazones - pharmacology; Medicine; Microbial Sensitivity Tests - methods; Pharmacology/Toxicology; Pharmacy; Research Article; Rhodanine - chemical synthesis; Rhodanine - pharmacology; Structure-Activity Relationship; 약학; Rhodanine; Antibacterial activity; Methicillin-resistant; Arylhydrazone; Quinolone-resistant
• ISSN: 0253-6269; 1976-3786
• DOI: 10.1007/s12272-013-0214-3

A series of arylhydrazone derivatives bearing a rhodanine moiety have been synthesized, characterized, and evaluated as antibacterial agents. Some of these compounds showed potent antibacterial activities against several different strains of Gram-positive bacteria, including multidrug-resistant clinical isolates. Of the compounds tested, IIk and IIIk were identified as the most effective, with minimum inhibitory concentration values of 2–4 μg/mL against multidrug-resistant Gram-positive organisms, including methicillin-resistant and quinolone-resistant Staphylococcus aureus . None of the compounds exhibited any activity against the Gram-negative bacteria Escherichia coli 1356 at 64 μg/mL.