Xun-Zhong Zou, An-Sheng Feng, Fu-Ran Zeng, Min-Cheng Lai, Yan-Zhi Liao, Meng Mei, Yu Li
Guangdong Research Center for Special Functional Building Materials and Its Green Preparation Technology, Foshan Research Center for Special Functional Building Materials and Its Green Preparation Technology, Guangdong Industry Polytechnic, Guangzhou 510006, China.
College of Light Industry and Food, Zhongkai University of Agriculture and Engineering, Guangzhou 510006, China.
Bioinorg Chem Appl. 2020 Sep 15;2020:8852470. doi: 10.1155/2020/8852470. eCollection 2020.
Two pyridine thiazole derivatives, namely, 4-(pyridin-2-yl)-2-(2-(pyridin-2-ylmethylene)hydrazinyl)thiazole (L1) and 4-(pyridin-3-yl)-2-(2-(pyridin-4-ylmethylene)hydrazinyl)thiazole (L2), were afforded by a cyclization reaction between -haloketone and thioamide, and their Zn(II) complexes were prepared by the reaction of ligands and corresponding metal salts, respectively, and characterized by X-ray diffraction and elemental analysis. Both crystals were obtained by ether diffusion and crystallized in a monoclinic system. The in vitro antimicrobial activity of the Zn(II) complexes and ligands was screened using the microplate reader method, and in vitro antitumor activities of the complexes were evaluated by MTT, with a view to developing new improved bioactive materials with novel properties. The biological activity studies of the compounds showed that the metal complexes were more active than the free ligands, and some compounds had absolute specificity for certain bacteria or cancer cell lines.
通过α-卤代酮与硫代酰胺之间的环化反应得到了两种吡啶噻唑衍生物,即4-(吡啶-2-基)-2-(2-(吡啶-2-基亚甲基)肼基)噻唑(L1)和4-(吡啶-3-基)-2-(2-(吡啶-4-基亚甲基)肼基)噻唑(L2),并分别通过配体与相应金属盐的反应制备了它们的Zn(II)配合物,通过X射线衍射和元素分析对其进行了表征。两种晶体均通过乙醚扩散获得,并在单斜晶系中结晶。使用微孔板读数器方法筛选了Zn(II)配合物和配体的体外抗菌活性,并通过MTT评估了配合物的体外抗肿瘤活性,以期开发具有新特性的新型改良生物活性材料。化合物的生物活性研究表明,金属配合物比游离配体更具活性,并且一些化合物对某些细菌或癌细胞系具有绝对特异性。