Synthesis and biological evaluation of 2-arylimino-3-pyridin-thiazolineone derivatives as antibacterial agents
Synthesis and biological evaluation of 2-arylimino-3-pyridin-thiazolineone derivatives as antibacterial agents
复制标题
抗菌剂2-芳基亚氨基-3-吡啶-噻唑啉酮衍生物的合成及生物学评价
DOI：
10.1016/j.bmcl.2016.03.089
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发表时间：
2016
影响因子：
2.7
通讯作者：
Chang Jun
中科院分区：
文献类型：
--
作者：
Cai Ming-Guang;Wu Yang;Chang Jun
为了寻找更有效的抗菌剂，合成了4个卤素二取代噻唑啉酮衍生物（2a-d）、5个卤素单取代噻唑啉酮衍生物（2 e-i）和11个2-芳基亚氨基-3-吡啶噻唑啉酮衍生物（2 j-t），并对其抗菌活性、杀菌活性、细胞毒性和红细胞溶血性进行了筛选。所合成的大部分衍生物对S.对Vero细胞的细胞毒性试验和对健康人红细胞的溶血活性试验表明，该制剂安全性好。2-芳基亚氨基-3-吡啶-噻唑啉酮衍生物不仅提高了葡萄球菌的logP值，而且对S.表皮病和MRSA。特别是几个化合物（2f、2 i、2 rand 2 t）表现出杀菌活性，其中化合物2 r在合成的化合物中表现出最好的抑制能力，进一步的可药性研究正在进行中。
With an intention to find more potent antibacterial agents, four halogen disubstituted thiazolineone derivatives (2a–d), five halogen monosubstituted thiazolineone derivatives (2e–i), and eleven 2-arylimino-3-pyridin-thiazolineone derivatives (2j–t) were synthesized and screened for their antibacterial activity, bactericidal activity, cytotoxicity, and erythrocyte hemolysis. Most of the synthesized derivatives showed antibacterial activity in inhibiting the growth ofS. epidermidisand MRSA, and exhibited safety in the cytotoxicity study on the Vero cells and hemolytic activities test on healthy human erythrocytes. 2-Arylimino-3-pyridin-thiazolineone derivatives not only improved theclogP, but also showed potent antibacterial activity in inhibiting the growth ofS. epidermidisand MRSA. In particularly, several compounds (2f,2i,2rand2t) showed bactericidal activity, in which compound2rdisplayed the best inhibitory capacity among the synthesized compounds, and further druggability research is on going.