Synthesis and antimicrobial evaluation of L-phenylalanine-derived C5-substituted rhodanine and chalcone derivatives containing thiobarbituric acid or 2-thioxo-4-thiazolidinone
Synthesis and antimicrobial evaluation of L-phenylalanine-derived C5-substituted rhodanine and chalcone derivatives containing thiobarbituric acid or 2-thioxo-4-thiazolidinone
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DOI：
10.1016/j.ejmech.2012.08.026
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发表时间：
2012-10-01
影响因子：
6.7
通讯作者：
Piao, Hu-Ri
中科院分区：
文献类型：
--
作者：
Jin, Xin;Zheng, Chang-Ji;Piao, Hu-Ri
设计、合成了l -苯丙氨酸衍生的c5取代罗丹宁（6a-q, 7a-j）和含有硫代巴比妥酸或2-硫氧-4-噻唑烷酮（9a-e, 11a-e）的查尔酮衍生物，并对其抗菌活性进行了表征和评价。其中部分化合物对革兰氏阳性菌，特别是对临床多药耐药菌株表现出明显的抑菌活性，其中化合物6c-e、6g、6i、6j和6q对金黄色葡萄球菌RN4220表现出较高的抑菌活性，最低抑菌浓度（MIC）为2 μ g/mL。化合物6q在所有化合物中对所有耐多药临床分离株的活性最强。然而，不幸的是，在64 μ g/mL时，没有一种化合物对革兰氏阴性菌有活性。(C) 2012 Elsevier Masson SAS。版权所有。
Four 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 mu g/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 mu g/mL. (C) 2012 Elsevier Masson SAS. All rights reserved.