C(2)-酰胺基-4-芳基-1,5-苯并硫氮杂的合成及抑菌活性的研究  

Synthesis and Antifungal Activity of 2-Carboxamide-4-aryl-1,5-benzothiazepines

作　　者：李文红[1,2] 张玲芬[1] 刘薇[3] 杜星琼[3] 李媛[1] 

机构地区：[1]河北师范大学化学与材料科学学院,石家庄050016 [2]河北工业职业技术学院环境与化学工程系,石家庄050091 [3]河北师范大学生命科学学院,石家庄050016

出　　处：《有机化学》2011年第8期1252-1257,共6页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.20972040);河北省自然科学基金(No.B2009000255)资助项目

摘　　要：设计合成了三类C(2)酰胺基取代的1,5-苯并硫氮杂衍生物:2-酰胺基(N-芳基)-4-芳基-1,5-苯并硫氮杂、2-酰胺基(N-烷基)-4-芳基-1,5-苯并硫氮杂和2-酰胺基(N,N-二烷基)-4-芳基-1,5-苯并硫氮杂,其结构用元素分析,IR,MS及1H NMR确证.测定了目标化合物的抑真菌活性,结果表明部分化合物对新生隐球菌具有中等强度的抑真菌活性.还研究了2-酰胺基-4-芳基-1,5-苯并硫氮杂的合成反应条件.Three kinds of 2-carboxamide-l,5-benzothiazepines including 2-carboxamide（N-aryl）-4-aryl, 2-carboxamide-（N-alkyl）-4-aryl and 2-carboxamide-（N,N-alkyl）-4-aryl-l,5-benzothiazepines were designed and synthesized, and their structures were characterized by elemental analysis, IR, 1H NMR, and MS tech- niques. Their antifungal activities against some fungi were evaluated, and the results indicated that some of them showed moderate fungicidal activities in vitro against C. neoformans. The synthesis conditions of the title compounds were also investigated.

关 键 词：1 5-苯并硫氮杂 酰胺 抑菌活性 

分 类 号：O626.32[理学—有机化学]