Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University, College of Pharmacy, Yanji City, Jilin Province 133002, PR China.
Eur J Med Chem. 2012 Aug;54:403-12. doi: 10.1016/j.ejmech.2012.05.023. Epub 2012 May 31.
Five series of (Z)-5-(4-(2-oxo-2-phenylethoxy)benzylidene)-2-thioxothiazolidin-4-one derivatives (I-V) were synthesized, characterized, and evaluated for their anti-bacterial activity. Most of the synthesized compounds showed potent inhibition against several Gram-positive bacteria (including multidrug-resistant clinical isolates) with MIC values in the range of 1-32 μg/mL. Compounds IIIi, Vb and Vc presented the most potent activity, showing four-fold more potency than norfloxacin (MIC = 8 μg/mL and 4 μg/mL) and 64-fold more activity than oxacillin (MIC > 64 μg/mL) against MRSA CCARM 3167 and 3506 strains with MIC values of 1 μg/mL, and 64-fold more potency than norfloxacin (MIC > 64 μg/mL) and comparable activity to oxacillin (MIC = 1 μg/mL) against the QRSA CCARM 3505 and 3519 strains. None of the compounds exhibited any activity against the Gram-negative bacteria Escherichia coli 1356 at 64 μg/mL.
合成了五组（Z）-5-（4-（2-氧代-2-苯乙氧基）亚苄基）-2-硫代噻唑烷-4-酮衍生物（I-V），并对其进行了表征和抗菌活性评价。大多数合成化合物对多种革兰氏阳性菌（包括多药耐药临床分离株）表现出很强的抑制作用，MIC 值在 1-32 μg/mL 范围内。化合物 IIIi、Vb 和 Vc 的活性最强，对 MRSA CCARM 3167 和 3506 株的 MIC 值为 1 μg/mL，分别比诺氟沙星（MIC = 8 μg/mL 和 4 μg/mL）和苯唑西林（MIC > 64 μg/mL）高 4 倍，对 QRSA CCARM 3505 和 3519 株的 MIC 值为 1 μg/mL，与苯唑西林（MIC = 1 μg/mL）相当，对革兰氏阴性菌大肠杆菌 1356 的 MIC 值为 64 μg/mL 时没有任何活性。
Zotero 插件