合成、抗菌和细胞毒性活性的一些新的噻唑俱乐部 1,3,4-噁二唑。
Synthesis, antimicrobial and cytotoxic activities of some novel thiazole clubbed 1,3,4-oxadiazoles.
机构信息
Division of Medicinal Chemistry, Department of Chemistry (DST-FIST Sponsored), Mahatma Gandhi Campus, Maharaja Krishnakumarsinhji Bhavnagar University, Bhavnagar 364 002, India.
出版信息
Eur J Med Chem. 2013 Sep;67:54-9. doi: 10.1016/j.ejmech.2013.06.029. Epub 2013 Jun 19.
A series of thiazole clubbed 1,3,4-oxadiazole derivatives (5a-l) have been synthesized and characterized by IR, (1)H NMR, (13)C NMR and mass spectral analysis. Synthesized compounds were evaluated for their antimicrobial and cytotoxic activities. The results indicated that, compounds 5c and 5i exhibited the most potent antibacterial activity. Compound 5f was found to be the most potent antifungal agent. The structure activity relationship revealed that the presence of electron withdrawing groups at para position of phenyl ring remarkably enhanced the antibacterial activity of synthesized compounds. Further, the results of preliminary MTT cytotoxicity studies on HeLa cells suggested that potent antimicrobial activity of 5b, 5c, 5f, 5h and 5i is accompanied by low cytotoxicity.
一系列噻唑并[5,4-d]嘧啶衍生物（5a-l）已被合成并通过红外光谱（IR）、（1）H NMR、（13）C NMR 和质谱分析进行了表征。合成的化合物被评估了其抗菌和细胞毒性活性。结果表明，化合物 5c 和 5i 表现出最强的抗菌活性。化合物 5f 被发现是最有效的抗真菌剂。结构活性关系表明，苯环对位上吸电子基团的存在显著增强了合成化合物的抗菌活性。此外，对 HeLa 细胞的初步 MTT 细胞毒性研究结果表明，5b、5c、5f、5h 和 5i 的强抗菌活性伴随着低细胞毒性。
Zotero 插件