Department of Chemistry, Faculty of Science, University of Malaya, Kuala Lumpur-50603, Malaysia.
Molecules. 2011 Jan 28;16(2):1297-309. doi: 10.3390/molecules16021297.
A series of 5-substituted-4-amino-1,2,4-triazole-3-thioesters was synthesized by converting variously substituted organic acids successively into the corresponding esters, hydrazides, 5-substituted-1,3,4-oxadiazole-2-thiols, 5-substituted-1,2,4-triazole-2-thiols and 5-substituted-1,3,4-oxadiazole-2-thioesters. Finally the target compounds were obtained by refluxing 5-substituted-1,3,4-oxadiazole-2-thioesters in the presence of hydrazine hydrate and absolute alcohol. The structures of the synthesized compounds were established by physicochemical and spectroscopic methods. The synthesized compounds were evaluated for their in vitro antifungal activity. Some of the evaluated compounds possessed significant antifungal activity as compared to a terbinafine standard.
将各种取代的有机酸依次转化为相应的酯、酰肼、5-取代-1,3,4-恶二唑-2-硫醇、5-取代-1,2,4-三唑-2-硫醇和 5-取代-1,3,4-恶二唑-2-硫代酯，合成了一系列 5-取代-4-氨基-1,2,4-三唑-3-硫酯。最后，在肼水和无水乙醇的存在下，将 5-取代-1,3,4-恶二唑-2-硫代酯回流，得到目标化合物。通过物理化学和光谱方法确定了合成化合物的结构。对合成化合物进行了体外抗真菌活性评价。与特比萘芬标准品相比，一些评价化合物具有显著的抗真菌活性。
