摘要/Abstract
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.
关键词: 1,5-苯并硫氮杂, 1,2,3-三氮唑, 抑真菌活性, 构效关系
Three kinds of 1,5-benzothiazepines containing 1,2,3-triazole, 3-(1H-1,2,3-triazolyl)-4-aryl-2,5-dihydro-1,5-benzo-thiazepines (5a~5f), 3-(2H-1,2,3-triazolyl)-4-aryl-2,3-dihydro-1,5-benzothiazepines (6a~6f) and 3-(1H-1,2,3-triazolyl)-4-aryl-2,3,4,5-tetrahydro-1,5-benzothiazepines (7a~7f), 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 5a~5f exhibited high inhibitory effects against fungi especially for Cryptococcus neoformans. The preliminary study on the structure-activity relationship of antifungal activity reveled that 1H-1,2,3-triazolyl and C=C double bond were the key function groups in the antifungal activity of 5a~5f.
Key words: 1,5-benzothiazepine, 1,2,3-triazole, antifungal activity, structure-activity relationship
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