| 论文题目: | 5-Benzylidenerhodanine and 5-benzylidene-2-4-thiazolidinedione based antibacterials |
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| 作者: | Zvarec, O; Polyak, SW; Tieu, W; Kuan, K; Dai, HQ; Pedersen, DS; Morona, R; Zhang, LX; Booker, GW; Abell, AD |
| 联系作者: | Abell, AD |
| 刊物名称: | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS |
| 期: | 8 |
| 卷: | 22 |
| 页: | 2720-2722 |
| 年份: | 2012 |
| 影响因子: | 2.554 |
| 论文下载: | |
| 摘要: | Herein we outline the antibacterial activity of amino acid containing thiazolidinediones and rhodanines against Gram-positive bacteria Staphylococcus aureus ATCC 31890, Staphylococcus epidermidis and Bacillus subtilis ATCC 6633. The rhodanine derivatives were generally more active than the analogous thiazolidinediones. Compounds of series 5 showed some selectivity for Bacillus subtilis ATCC 6633, the extent of which is enhanced by the inclusion of a non-polar amino acid at the 5-position of the core thiazolidinediones and rhodanines scaffolds. SAR data of series 8 demonstrated improved activity against the clinically more significant Staphylococci with selectivity over Bacillus subtilis ATCC 6633 induced by introduction of a bulky aryl substituent at the 5-position of the core scaffolds. (C) 2012 Elsevier Ltd. All rights reserved. |
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