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Ru(ii)-N-heterocyclic carbene complexes: synthesis, characterization, transfer hydrogenation reactions and biological determination

机译：Ru（ii）-N-杂环卡宾络合物：合成，表征，转移氢化反应和生物学测定

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A series of ruthenium(ii) complexes with N-heterocyclic carbene ligands were successfully synthesized by transmetalation reactions between silver(i) N-heterocyclic carbene complexes and [RuCl2(p-cymene)](2) in dichloromethane under Ar conditions. All new compounds were characterized by spectroscopic and analytical methods. These ruthenium(ii)-NHC complexes were found to be efficient precatalysts for the transfer hydrogenation of ketones by using 2-propanol as the hydrogen source in the presence of KOH as a co-catalyst. The antibacterial activity of ruthenium N-heterocyclic carbene complexes 3a-f was measured by disc diffusion method against Gram positive and Gram-negative bacteria. Compounds 3d exhibited potential antibacterial activity against five bacterial species among the six used as indicator cells. The product 3e inhibits the growth of all the six tested microorganisms. Moreover, the antioxidant activity determination of these complexes 3a-f, using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2 '-azinobis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS) as reagent, showed that compounds 3b and 3d possess DPPH and ABTS antiradical activities. From a concentration of 1 mg ml(-1), these two complexes presented a similar scavenging activity to that of the two used controls gallic acid (GA) and butylated hydroxytoluene (BHT). From a concentration of 10 mg ml(-1), the percentage inhibition of complexes 3b and 3d was respectively 70% and 90%. In addition, these two Ru-NHC complexes exhibited antifungal activity against Candida albicans. Investigation of the anti-acetylcholinesterase activity of the studied complexes showed that compounds 3a, 3b, 3d and 3e exhibited good activity at 100 mu g ml(-1) and product 3d is the most active. In a cytotoxicity study the complexes 3 were evaluated against two human cancer cell lines MDA-MB-231 and MCF-7. Both 3d and 3e complexes were found to be active against the tested cell lines showing comparable activity with examples in the literature.
机译：通过在Ar条件下的二氯甲烷中的透射率反应和在Ar条件下，通过在Ar条件下的二氯甲烷中的透射反应成功地合成了一系列具有正杂环配体的钌（II）络合物。甲基甲烷中的[RuCl 2（p-Cymene）]（2）。所有新化合物都是通过光谱和分析方法的特征。发现这些钌（II）-NHC复合物在KOH作为助催化剂存在下，通过使用2-丙醇作为氢源，以有效的预催化剂用于通过使用2-丙醇作为氢源转移酮。通过对革兰氏阳性和革兰氏阴性细菌的盘扩散法测量钌N-杂环卡宾络合物3A-F的抗菌活性。化合物3D在用作指示细胞中的六个细菌种类上表现出潜在的抗菌活性。产品3E抑制所有六种测试的微生物的生长。此外，使用2,2-二苯基-1-富铬酰基（DPPH）和2,2'-Sazinobis-3-乙基苯并噻唑啉-6-磺酸（ABTS）作为试剂的抗氧化活性测定这些配合物3A-F的抗氧化活性测定。化合物3B和3D具有DPPH和ABTS抗动图活动。从1mg ml（-1）的浓度，这两种络合物向两种使用的对照对无菌（Ga）和丁基化羟基甲苯（BHT）的两种使用的对照呈现类似的清除活性。从10mg ml（-1）的浓度，络合物3b和3d的抑制率分别为70％和90％。此外，这两种Ru-NHC综合体表现出对念珠菌蛋白糖苷的抗真菌活性。研究了所研究的复合物的抗乙酰胆碱酯酶活性的研究表明，化合物3a，3b，3d和3e在100μgmml（-1）中表现出良好的活性，并且产品3D是最活跃的。在一种细胞毒性研究中，将复合物3对两种人类癌细胞系MDA-MB-231和MCF-7进行评估。发现3D和3E复合物均针对测试的细胞系有效，所述细胞系显示与文献中的实例相当的活性。

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    《RSC Advances》 |2019年第59期|共15页
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