含1,2,3-三氮唑结构的1,5-苯并硫氮杂[艹卓]的合成及其抑真菌活性

设计合成了三类含1,2,3-三氮唑结构的1,5-苯并硫氮杂艹卓]化合物3-(1H-1,2,3-三氮唑)-4-芳基-2,5-二氢-1,5-苯并硫氮杂艹卓](5a^5f)、3-(2H-1,2,3-三氮唑)-4-芳基-2,3-二氢-1,5-苯并硫氮杂艹卓](6a^6f)和3-(1H-1,2,3-三氮唑)-4-芳基-2,3,4,5-四氢-1,5-苯并硫氮杂艹卓](7a^7f).研究了中间体及目标产物的合成条件,分离出其中两个副产物并进行了结构确定.目标产物的抑真菌活性测试表明,化合物5a^5f对真菌具有良好的抑制作用,对新生隐球菌的抑制效果尤为突出.初步抑真菌构效关系研究表明, 1H-1,2,3-三氮唑环和C=C双键是化合物5a^5f抑真菌活性的关键官能团.

Synthesis and Antifungal Activity of 1,5-Benzothiazepines Containing 1,2,3-Triazole

Three kinds of 1,5-benzothiazepines containing 1,2,3-triazole, 3-(1 H-1,2,3-triazolyl)-4-aryl-2,5-dihydro-1,5-benzothiazepines(5 a^5 f), 3-(2 H-1,2,3-triazolyl)-4-aryl-2,3-dihydro-1,5-benzothiazepines(6 a^6 f) and 3-(1 H-1,2,3-triazolyl)-4-aryl-2,3,4,5-tetrahydro-1,5-benzothiazepines(7 a^7 f), were designed and synthesized. The synthesis conditions of intermediates and target products were studied. Two by-products were separated and their structures were determined. The antifungal activity test of the target products showed that compounds 5 a^5 f exhibited high inhibitory effects against fungi especially for Cryptococcus neoformans. The preliminary study on the structure-activity relationship of antifungal activity reveled that 1 H-1,2,3-triazolyl and C=C double bond were the key function groups in the antifungal activity of 5 a^5 f.