Abstract

The first ever synthesis of complexes [PdLCl₂] (I) and [PdLBr₂] (II) was successfully achieved, where L = 2,6-dimethyl-4-nitro-N-(pyridin-2-ylmethylildene)aniline, a ligand with a purported ability to inhibit monoamine oxidase B (MAO-B). To gain insight into the molecular structure of complexes I and II, as well as the ligand precursor 2,6-dimethyl-4-nitroaniline L⁴ (CIF files CCDC nos. 2255106 (I), 2255105 (II), 2255103 (L), 2255104 (L⁴)), X-ray diffraction analysis was utilized. Complex I underwent further characterization to determine its stability, solubility, and lipophilicity. Cytotoxicity studies of substances L, I, and II on human embryonic kidney cell line HEK-293 showed no evidence of cytotoxic activity. To evaluate the inhibitory activity of new substances L, I, and II as well as established substances III−IX, selegiline, and rasagiline, ex vivo studies were conducted, establishing a structure/activity relationship.

中文翻译：

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Pd(II) 的硝基取代吡啶亚胺配合物：离体 MAO-B 的合成和抑制

摘要

首次成功合成了配合物 [PdLCl ₂ ] ( I ) 和 [PdLBr ₂ ] ( II )，其中 L = 2,6-二甲基-4-硝基-N- (吡啶-2-基亚甲基)苯胺，据称具有抑制单胺氧化酶 B (MAO-B) 能力的配体。深入了解配合物I和 II以及配体前体 2,6-二甲基-4-硝基苯胺 L ⁴的分子结构（CIF 文件 CCDC 编号 2255106 ( I )、2255105 ( II )、2255103 (L) ，2255104 (L ⁴ ))，利用X射线衍射分析。复合物I进行了进一步的表征以确定其稳定性、溶解度和亲脂性。物质 L、I和II对人胚胎肾细胞系 HEK-293 的细胞毒性研究显示没有细胞毒性活性的证据。为了评估新物质 L、 I和II以及已确定的物质III – IX、司来吉兰和雷沙吉兰的抑制活性，进行了离体研究，建立了结构/活性关系。