3-苯甲酰基/亚甲基取代的1,5-苯并硫氮杂艹卓化合物的合成及抑菌活性  

Synthesis and Antimicrobial Activity of 3-benzoyl/methylene Substituted 1,5-benzothiazepines

作　　者：鲁佳琪 王娇 张磊 张萍[1] LU Jiaqi;WANG Jiao;ZHANG Lei;ZHANG Ping(College of Chemistry and Materials Science,Hebei Normal University,HebeiShijiazhuang 050024,China;Chengde Xinglong County No.1 Middle School,HebeiChengde 067399,China)

机构地区：[1]河北师范大学化学与材料科学学院,河北石家庄050024 [2]承德市兴隆县第一中学,河北承德067399

出　　处：《河北师范大学学报（自然科学版）》2024年第5期477-483,共7页Journal of Hebei Normal University：Natural Science

基　　金：国家自然科学基金(21801059);河北省自然科学基金(B2017205100)。

摘　　要：以1-芳基-3-N,N-二甲胺基-1-丙酮盐酸盐(Ⅰa~f)为起始原料,经过取代反应、曼尼希反应和亲核加成反应合成了3位含有苯甲酰基和亚甲基取代的1,5-苯并硫氮杂䓬化合物Ⅳa~f和Ⅴa~f.通过^(1)HNMR,^(13)CNMR,MS和元素分析对Ⅳa~f和Ⅴa~f的结构进行了确证,并测试了其对真菌和细菌的抑制作用.结果显示,化合物Ⅳb对白色念珠菌和新生隐球菌标准株具有轻度的抑制作用.3-benzoyl/methylene substituted 1,5-benzothiazepine compounds Ⅳa~f and Ⅴa~f were synthesized through substitution reaction, Mannich reaction and nucleophilic addition reaction using 1-aryl-3-N,N-dimethylamino-1-acetone hydrochloride(Ⅰa~f) as the starting materials.The structures of Ⅳa~f and Ⅴa~f were characterized by ~1HNMR,~(13)CNMR,MS and elemental analysis.And the inhibitory effects of compounds Ⅳa~f and Ⅴa~f on fungi and bacteria were tested.The results showed that compound Ⅳb had slight inhibitory effect on Candida albicans and Cryptococcus neoformans stand.

关 键 词：3-苯甲酰基-1 5-苯并硫氮杂䓬 3-亚甲基-1 5-苯并硫氮杂䓬 曼尼希反应 抑菌活性 

分 类 号：O622.6[理学—有机化学]