新型 5-(2-噻吩基)-1,2,4-三唑和 5-(2-噻吩基)-1,3,4-恶二唑及其相关衍生物的合成与抗菌活性。
Synthesis and antimicrobial activity of new 5-(2-thienyl)-1,2,4-triazoles and 5-(2-thienyl)-1,3,4-oxadiazoles and related derivatives.
机构信息
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
出版信息
Molecules. 2010 Jan 22;15(1):502-14. doi: 10.3390/molecules15010502.
New 5-(2-thienyl)-1,2,4-triazoles and 5-(2-thienyl)-1,3,4-oxadiazoles namely, N-[3-mercapto-5-(2-thienyl)-1,2,4-triazol-4-yl]-N'-arylthioureas 4a-e, 2-arylamino-5-(2-thienyl)-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles 5a-e, 3-arylaminomethyl-5-(2-thienyl)-1,3,4-oxadiazoline-2-thiones 7a-e, 3-(N-substituted anilinomethyl)-5-(2-thienyl)-1,3,4-oxadiazoline-2-thiones 8a, b and 3-(4-substituted-1-piperazinylmethyl)-5-(2-thienyl)-1,3,4-oxadiazoline-2-thiones 9a-f, were prepared. The synthesized compounds were tested for in vitro activities against certain strains of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. Compound 9a displayed marked broad spectrum antibacterial activity, while compounds 4d, 5e, 7b, 7c, 7d, 9b, 9c and 9d were highly active against the tested Gram-positive bacteria. None of the synthesized compounds were proved to be significantly active against Candida albicans.
新的 5-(2-噻吩基)-1,2,4-三唑和 5-(2-噻吩基)-1,3,4-恶二唑，即 N-[3-巯基-5-(2-噻吩基)-1,2,4-三唑-4-基]-N'-芳基硫脲 4a-e、2-芳基氨基-5-(2-噻吩基)-1,2,4-三唑并[3,4-b][1,3,4]噻二唑 5a-e、3-芳基甲胺基-5-(2-噻吩基)-1,3,4-恶二唑啉-2-硫酮 7a-e、3-(N-取代芳基甲胺基)-5-(2-噻吩基)-1,3,4-恶二唑啉-2-硫酮 8a,b 和 3-(4-取代-1-哌嗪基甲胺基)-5-(2-噻吩基)-1,3,4-恶二唑啉-2-硫酮 9a-f，均被制备出来。这些合成的化合物被测试了对革兰氏阳性和革兰氏阴性细菌以及酵母样致病真菌白色念珠菌的体外活性。化合物 9a 表现出显著的广谱抗菌活性，而化合物 4d、5e、7b、7c、7d、9b、9c 和 9d 对测试的革兰氏阳性菌具有高度的活性。没有一个合成的化合物被证明对白色念珠菌有显著的活性。
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