Organic Research Laboratory, Department of Bioresources and Food Science, College of Life and Environmental Sciences, Konkuk University, Seoul 143 701, South Korea.
Eur J Med Chem. 2014 Jan;71:24-30. doi: 10.1016/j.ejmech.2013.10.059. Epub 2013 Nov 1.
As an aspect of our ongoing research in search of new antimicrobial armamentarium, a series of 1,2,4-triazol-3-ylthio-acetamides was constructed and in vitro analyzed for their antimicrobial activity against several bacteria and fungi. Aiming to establish an increased potency, the bioassay results were matched to those of 1,3,4-oxadiazoles, utilized previously. Remarkably, 1,2,4-triazoles were found to possess a good spectrum of antifungal potency, which eventually suggested the azole template as an essential pharmacophore to diversify the biological occupations of the attendant molecules. However, it was noticed that the potency of final analogs against each strain placed reliance on the type of substituent present on benzothiazole ring. The structures of final compounds were confirmed with the aid of IR, (1)H NMR, (13)C NMR spectroscopy and CHN analysis.
作为我们正在进行的寻找新抗菌武器研究的一个方面,我们构建了一系列 1,2,4-三唑-3-巯基乙酰胺,并对其进行了体外分析,以评估它们对几种细菌和真菌的抗菌活性。为了提高活性,我们将生物测定结果与之前使用的 1,3,4-恶二唑进行了匹配。值得注意的是,1,2,4-三唑具有良好的广谱抗真菌活性,这最终表明唑类模板是多样化相关分子生物学作用的必需药效团。然而,我们注意到,最终类似物对每种菌株的活性取决于苯并噻唑环上存在的取代基的类型。最终化合物的结构通过红外光谱(IR)、(1)H NMR、(13)C NMR 光谱和 CHN 分析得到了确认。