Synthesis and antibacterial evaluation of rhodanine-based 5-aryloxy pyrazoles against selected methicillin resistant and quinolone-resistant Staphylococcus aureus (MRSA and QRSA)
Synthesis and antibacterial evaluation of rhodanine-based 5-aryloxy pyrazoles against selected methicillin resistant and quinolone-resistant Staphylococcus aureus (MRSA and QRSA)
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DOI：
10.1016/j.ejmech.2012.12.007
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发表时间：
2013-02-01
影响因子：
6.7
通讯作者：
Piao, Hu-Ri
中科院分区：
文献类型：
--
作者：
Song, Ming-Xia;Zheng, Chang-Ji;Piao, Hu-Ri
为了提高5-芳氧基吡唑和绕丹宁衍生物的抗菌活性，合成了8个系列的杂合化合物，并对其抗菌活性进行了评价。大多数合成的化合物对选定的耐甲氧西林和耐喹诺酮金黄色葡萄球菌（MRSA，QRSA）显示出良好的抑制活性，最小抑制浓度（MIC）值在1-32 μ g/mL的范围内。细胞毒性试验表明，这些化合物在非细胞毒性浓度下表现出体外抗菌活性。因此，这些研究表明，绕丹宁基5-芳氧基吡唑是有趣的支架，用于开发新的革兰氏阳性抗菌剂。(C)2012年Elsevier Masson SAS。All rights reserved.
With an intention to synergize the anti-bacterial activity of 5-aryloxy pyrazole and rhodanine derivatives, eight series of hybrid compounds have been synthesized and evaluated for their antibacterial activity. The majority of the synthesized compounds showed good inhibitory activity against selected methicillin resistant and quinolone-resistant Staphylococcus aureus (MRSA, QRSA) with minimum inhibitory concentration (MIC) values in the range of 1-32 mu g/mL. The cytotoxicity test suggests that these compounds exhibited in vitro antibacterial activity at non-cytotoxic concentrations. These studies therefore suggest that rhodanine-based 5-aryloxy pyrazoles are interesting scaffolds for the development of novel Gram-positive antibacterial agents. (C) 2012 Elsevier Masson SAS. All rights reserved.