Girish V, Khanum Noor Fatima, Gurupadaswamy H D, Khanum Shaukath Ara
Bioorg Khim. 2014 May-Jun;40(3):357-62.
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.
阐述了十种新型2-[2-(芳酰基)芳酰氧基]甲基-1,3,4-恶二唑作为新型潜在抗菌剂的合成途径。用原甲酸三乙酯使2-(2-芳酰基芳氧基)乙酰肼分子内环化生成2-[2-(芳酰基)芳酰氧基]甲基-1,3,4-恶二唑，产率良好。通过红外光谱、1H核磁共振、质谱以及元素分析对这些化合物进行了表征。采用纸片扩散法和微量稀释法对目标化合物针对代表性菌株的体外抗菌活性进行了测试。几种化合物显示出与标准药物相当或更高的抗菌活性。
