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Synthesis, physicochemical properties and antimicrobial activity of some new benzimidazole derivatives.

机译:一些新的苯并咪唑衍生物的合成,理化性质和抗菌活性。

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摘要

Some derivatives of benzimidazole were synthesized by nucleophilic substitution of 2-substituted-1H-benzimidazole. The resulting ethyl (2-substituted-1H-benzimidazol-1-yl) acetate on treatment with hydrazine hydrate yielded 2-(2-substituted-1H-benzimidazol-1-yl) acetohydrazide, which on further reaction with one equivalent of different aliphatic or aromatic carboxylic acids in the presence of phosphoryl chloride afforded the corresponding target compounds, 2-substituted-1-[{(5-substituted alkyl/aryl)-1,3,4-oxadiazol-2-yl} methyl]-1H-benzimidazole. The structures of the synthesized compounds were evaluated by spectral and elemental methods of analyses. All the synthesized compounds were screened for their antimicrobial activities. All of the derivatives showed good activity towards Gram-positive bacteria and negligible activity towards Gram-negative bacteria. Some of the synthesized compounds showed moderate activity against tested fungi.
机译:通过2-取代-1H-苯并咪唑的亲核取代反应合成了一些苯并咪唑的衍生物。用水合肼处理所得的(2-取代的-1H-苯并咪唑-1-基)乙酸乙酯,得到2-(2-取代的-1H-苯并咪唑-1-基)乙酰肼,其与一当量的不同脂肪族化合物进一步反应。或在磷酰氯存在下的芳族羧酸得到相应的目标化合物,2-取代-1-[{((5-取代烷基/芳基)-1,3,4-恶二唑-2-基}甲基] -1H-苯并咪唑。合成化合物的结构通过光谱和元素分析法进行评估。筛选所有合成的化合物的抗菌活性。所有的衍生物对革兰氏阳性菌均表现出良好的活性,而对革兰氏阴性菌则表现出可忽略的活性。一些合成的化合物显示出对测试真菌的中等活性。

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