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首页> 外文期刊>American Journal of Drug Discovery and Development >Synthesis and Evaluation of Diorganotin(IV) and Triorganotin(IV) Derivatives of Aspirin, Paracetamol and Metronidazole as Antimicrobial Agents
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Synthesis and Evaluation of Diorganotin(IV) and Triorganotin(IV) Derivatives of Aspirin, Paracetamol and Metronidazole as Antimicrobial Agents

机译：阿司匹林，扑热息痛和甲硝唑作为抗菌剂的二有机锡（IV）和三有机锡（IV）衍生物的合成与评价

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A large number of organotin complexes are used as pharmaceuticals, pesticides, stabilizers and fire retardants. In an attempt to explore its pharmaceutical profile, new diorganotin (IV) R2SnA2 (R = n-Bu, n-Oct) and triorganotin (IV) R3SnA2 (R= n-Bu) derivatives where A is the anion of 2-acetoxybenzoic acid (Aspirin), N-(4-hydroxyphenyl) acetamide (Paracetamol) and 2-(2-methyl-5-nitroimidazol-1-yl) ethanol (Metronidazole) have been synthesized. The complexes 1-9 were characterized by elemental analysis as well as FTIR, nuclear magnetic resonance (1H, 13C and 119Sn) spectroscopy. On the basis of these spectroscopic studies it is proposed that diorganotin complexes of Paracetamol and Metronidazole having 1:2 stoichiometry, show tetrahedral geometry while the complexes of Aspirin show octahedral arrangement around tin metal ion with bi-dentate nature of carboxylate group. Triorganotin complexes of Aspirin, Paracetamol and Metronidazole having 1:2 stoichiometry show trigonal bipyramidal geometry with monodentate nature of the carboxylate group around the organotin moiety in the complexes of Aspirin. The ligand molecules bound to the Sn atom through carboxyl oxygen atoms in Aspirin and hydroxyl oxygen in Paracetamol and Metronidazole. The anti-fungal activity of complexes 1, 4 and 9 has been determined against Candida albicans. It is observed that the activity increases on complexation and highest antifungal activity has been found for the triorganotin complex of metronidazole.
机译：大量的有机锡配合物被用作药物，农药，稳定剂和阻燃剂。为了探索其药物特性，新的二有机锡（IV）R2SnA2（R = n-Bu，n-Oct）和三有机锡（IV）R3SnA2（R = n-Bu）衍生物，其中A是2-乙酰氧基苯甲酸的阴离子合成了（阿司匹林），N-（4-羟苯基）乙酰胺（扑热息痛）和2-（2-甲基-5-硝基咪唑-1-基）乙醇（甲硝唑）。通过元素分析，FTIR，核磁共振（1H，13C和119Sn）光谱对配合物1-9进行表征。根据这些光谱学研究，提出扑热息痛和甲硝唑的二有机锡配合物具有1：2的化学计量比，显示出四面体的几何形状，而阿司匹林的配合物在锡金属离子周围显示出八面体的排列，具有羧酸根的双齿性质。化学计量比为1：2的阿司匹林，扑热息痛和甲硝唑的三有机锡复合物显示出三角形的双锥体几何结构，其阿斯匹林复合物中有机锡部分周围的羧酸酯基具有单齿性质。配体分子通过阿司匹林中的羧基氧原子和扑热息痛和甲硝唑中的羟基氧与Sn原子结合。已经确定了复合物1、4和9的抗真菌活性对白色念珠菌。观察到在络合时活性增加，并且已经发现甲硝唑的三有机锡复合物具有最高的抗真菌活性。

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