Synthesis and evaluation of in vitro antimicrobial activity of novel 2-[2-(aroyl)aroyloxy]methyl-1,3,4-oxadiazoles.

Bioorganicheskaia khimiia Pub Date : 2014-05-01
V Girish, Noor Fatima Khanum, H D Gurupadaswamy, Shaukath Ara Khanum
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Abstract

Synthetic pathway of the ten novel 2-[2-(aroyl)aroyloxy]methyl-1,3,4-oxadiazoles as new potential antimicrobial agents is illustrated. Intramolecular cyclization of 2-(2-aroylaryloxy) aceto hydrazides to 2-[2-(aroyl)aroyloxy]methyl-1,3,4-oxadiazoles was achieved with triethyl orthoformate in good yields. The compounds were characterized by IR, 1H NMR, mass spectra and by means of CHN analysis. The target compounds were tested for their in vitro antimicrobial activity against representative strains by disc diffusion method and micro dilution methods. Several compounds showed antimicrobial activity comparable with or higher than the standard drugs.

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新型2-[2-(芳基)芳氧基]甲基-1,3,4-恶二唑的合成及体外抗菌活性评价。
介绍了10种新型抗菌药物2-[2-(芳基)芳氧基]甲基-1,3,4-恶二唑的合成途径。以原甲酸三乙酯为原料,实现了2-(2-芳基芳氧基)乙酰肼分子内环化成2-[2-(芳基)芳氧基]甲基-1,3,4-恶二唑的反应。通过IR、1H NMR、质谱和CHN分析对化合物进行了表征。采用圆盘扩散法和微量稀释法测定目标化合物对代表性菌株的体外抑菌活性。几种化合物显示出与标准药物相当或高于标准药物的抗菌活性。
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