Department of Industrial Chemistry, Alagappa University, Karaikudi 630 003, Tamil Nadu, India.
Eur J Med Chem. 2011 Nov;46(11):5465-72. doi: 10.1016/j.ejmech.2011.09.007. Epub 2011 Sep 10.
A series of mono and bis-1,2,3-selenadiazole derivatives have been synthesized by the oxidative cyclization of mono and bis semicarbazones of 2-(3-oxo-1,3-diarylpropyl)-1-cyclohexanones using selenium(IV) oxide. The newly synthesized compounds were evaluated for their in vitro antimicrobial activity against Escherichia coli (ATCC 25922), Staphylococcus aureus (ATCC 11632) and Candida albicans (ATCC 90028) and in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv (MTB). Among these compounds, 1,3-di(4-chlorophenyl)-3-(4,5,6,7-tetrahydro-1,2,3-benzoselenadiazol-4-yl)-1-propanone (2h) and 3-(4-chlorophenyl)-1-(4-methylphenyl)-3-(4,5,6,7-tetrahydro-1,2,3-benzoselenadiazol-4-yl)-1-propanone (2g) were found to be the most active compounds with MIC of 3.3 and 3.5 μM respectively against MTB.
一系列的单和双-1,2,3-硒二唑衍生物已经通过使用氧化硒（IV）氧化 2-(3-氧代-1,3-二芳基丙基）-1-环己酮的单和双缩氨基脲的环氧化合来合成。新合成的化合物对大肠杆菌（ATCC 25922）、金黄色葡萄球菌（ATCC 11632）和白色念珠菌（ATCC 90028）的体外抗菌活性进行了评估，并对结核分枝杆菌 H37Rv（MTB）的体外抗结核活性进行了评估。在这些化合物中，1,3-二（4-氯苯基）-3-（4,5,6,7-四氢-1,2,3-苯并硒二唑-4-基）-1-丙酮（2h）和 3-（4-氯苯基）-1-（4-甲基苯基）-3-（4,5,6,7-四氢-1,2,3-苯并硒二唑-4-基）-1-丙酮（2g）被发现是最有效的化合物，对 MTB 的 MIC 分别为 3.3 和 3.5 μM。
