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Biological activity of two novel zinc(II) complexes with NSAID mefenamic acid
Chemical Papers ( IF 2.1 ) Pub Date : 2019-11-27 , DOI: 10.1007/s11696-019-01003-5
Romana Smolková , Vladimír Zeleňák , Róbert Gyepes , Daniela Hudecová

Zinc(II) mefenamate [Zn(mef)2] (1) along with two novel Zn(II) crystalline complexes with Hmef (mefenamic acid) [Zn(dmso)2(mef)2] (2) and [Zn(cyclam)(mef)2] (3) were synthesized and characterized by infrared spectroscopy, elemental and thermal analysis. Crystal structures of complexes 2 and 3 were determined by single-crystal X-ray structure analysis. The biological activity of complexes was investigated using various methods. First, the ability of the complexes to scavenge radicals [2,2-diphenyl-1-picrylhydrazyl—DPPH and diammonium 2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonate)—ABTS] was investigated, indicating selective scavenging activity of studied compounds for ABTS·+ in comparison to DPPH·. The complexes 2 and 3 are more active than the free Hmef. Second, the interaction of the complexes with serum albumins was investigated and obtained binding constants are within optimal range for transport in bloodstream. Third, the interaction of complexes with fish sperm DNA (FS-DNA) was studied by UV–Vis titration and competitive binding studies with ethidium bromide (EB). The obtained values of binding constants calculated from UV–Vis measurements and fluorescence measurements, respectively, indicates the strongest binding for complex 3. Fourth, antimicrobial activity of compounds 13 was studied against bacteria (S. aureus and E. coli), yeast (C. parapsilosis) and filamentous fungi (R. oryzae, A. alternata, M. gypseum); complex 1 indicates highest activity against filamentous fungi R. oryzae and A. alternate whereas complex 2 displays highest antimicrobial activity against both Gram-positive and Gram-negative bacteria and yeast.

中文翻译:

NSAID甲芬那酸的两种新型锌(II)配合物的生物活性

甲芬那酸锌(II)[Zn(mef2 ](1)以及两个具有H mef(甲芬那酸)[Zn(dmso2mef2 ](2)和[Zn(合成了Cyclam)(mef2 ](3)并通过红外光谱,元素和热分析对其进行了表征。配合物23的晶体结构通过单晶X射线结构分析确定。使用多种方法研究了复合物的生物活性。首先,研究了该络合物清除自由基[2,2-二苯基-1-吡啶并肼基-DPPH和2,2'-叠氮基双(3-乙基苯并噻唑啉-6-磺酸盐)-ABTS二铵]的能力,表明了选择性清除作用与DPPH ·相比,所研究化合物对ABTS ·+的活性较高。配合物23比自由H mef更具活性。其次,研究了复合物与血清白蛋白的相互作用,获得的结合常数在血流运输的最佳范围内。第三,通过UV-Vis滴定和与溴化乙锭(EB)的竞争结合研究,研究了配合物与鱼精DNA(FS-DNA)的相互作用。分别从UV-Vis测量和荧光测量计算得到的结合常数值表明对复合物3的最强结合。第四,化合物的抗微生物活性1 - 3进行了研究对细菌(金黄色葡萄球菌大肠杆菌),酵母(近平滑念珠菌)和丝状真菌(米根霉A. alternataM.石膏); 复杂1指示针对丝状真菌活性最高米根霉A.备用而复杂2只显示针对革兰氏阳性和革兰氏阴性细菌和酵母都最高的抗菌活性。
更新日期:2019-11-27
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