Abstract

Synthesis and characterization of novel copper complexes of metronidazole benzoate (MTZ Benz), metronidazole (MTZ) in the presence of another ligand; dichloroacetic acid (DCA) were compared and reported in the present work. Different bacterial and fungus strains were ascertained to evaluate the biological potency of the synthesized complexes, that is, Escherichia coli, Bordetella bronceptica, Staphylococcus epidermidis, Baccilus pumilus, Staphylococcus aureus and yeast strain Saccharomyces cerevisiae. Agar diffusion method was employed to investigate in vitro antibacterial activities of the synthesized metal complexes and the tested parent ligands. α-Amylase and α-glucosidase inhibition studies of the synthesized complexes were also carried out. The antibacterial potential and α-amylase and α-glucosidase inhibition studies of complexes were further investigated by molecular docking studies, which supported the experimental results. Significant α-amylase and α-glucosidase inhibition activities were shown by the synthesized complexes. S-1 and S-5 were found to be most inhibitors of α-amylase and α-glucosidase having IC₅₀ 42.50, 44.80 and 4.52 µg/mL, 4.80 µg/mL, respectively. The newly synthesized copper complexes showed overall better biological activities compared to each parent ligands used.

Communicated by Ramaswamy H. Sarma

摘要

在另一种配体存在下，合成了甲硝唑苯甲酸酯（MTZ Benz），甲硝唑（MTZ）的新型铜配合物并进行了表征；比较了二氯乙酸（DCA），并在当前工作中进行了报道。确定了不同的细菌和真菌菌株以评估合成的复合物的生物学效价，即大肠杆菌，Brodetella bronceptica，表皮葡萄球菌，短小芽孢杆菌，金黄色葡萄球菌和酵母菌株啤酒酵母。琼脂扩散法用于体外研究合成的金属配合物和测试的母体配体的抗菌活性。还对合成的复合物进行了α-淀粉酶和α-葡萄糖苷酶抑制研究。通过分子对接研究进一步研究了复合物的抗菌潜力以及对α-淀粉酶和α-葡萄糖苷酶的抑制作用，为实验结果提供了支持。合成的配合物显示出显着的α-淀粉酶和α-葡萄糖苷酶抑制活性。发现S-1和S-5是大多数α-淀粉酶和α-葡萄糖苷酶抑制剂，IC _50分别为42.50、44.80和4.52 µg / mL，4.80 µg / mL。与使用的每个母体配体相比，新合成的铜络合物总体上显示出更好的生物活性。

由Ramaswamy H.Sarma沟通