Xin Jin, Chang-Ji Zheng, Ming-Xia Song, Yan Wu, Liang-Peng Sun, Yin-Jing Li, Li-Jun Yu, Hu-Ri Piao
Institute of Pharmaceutical Chemistry and Pharmacology, Inner Mongolia University for Nationalities, Tongliao, Inner Mongolia Autonomous Region, 028002, PR China.
European journal of medicinal chemistry 2012 OctFour novel series of compounds, including the l-phenylalanine-derived C5-substituted rhodanine (6a-q, 7a-j) and chalcone derivatives containing thiobarbituric acid or 2-thioxo-4-thiazolidinone (9a-e, 11a-e) have been designed, synthesized, characterized, and evaluated for their antibacterial activity. Some of these compounds showed significant antibacterial activity against Gram-positive bacterias, especially against the strains of multidrug-resistant clinical isolates, among which compounds 6c-e, 6g, 6i, 6j and 6q exhibiting high levels of antimicrobial activity against Staphylococcus aureus RN4220 with minimum inhibitory concentration (MIC) values of 2 μg/mL. Compound 6q showed the most potent activity of all of the compounds against all of the test multidrug-resistant clinical isolates tested. Unfortunately, however, none of the compounds were active against Gram-negative bacteria at 64 μg/mL. Copyright © 2012 Elsevier Masson SAS. All rights reserved.
Xin Jin, Chang-Ji Zheng, Ming-Xia Song, Yan Wu, Liang-Peng Sun, Yin-Jing Li, Li-Jun Yu, Hu-Ri Piao. Synthesis and antimicrobial evaluation of L-phenylalanine-derived C5-substituted rhodanine and chalcone derivatives containing thiobarbituric acid or 2-thioxo-4-thiazolidinone. European journal of medicinal chemistry. 2012 Oct;56:203-9
PMID: 22982124
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