Synthesis And Antimicrobial Activity Of 3-CH₂CH₂COOCH₃ Substituted/ Oxadiazolo (5,4-d)(1,5)Benzothiazepines

1,5-benzothiazepine is a kind of compound which has important physiological activities. Some of its derivatives have been used in clinic as antianxiety drugs, hyprosis and cardiovascular medicines. Therefore, its syntheses, structures and pharmacological activities have been attracted wide attentions.By now, a variety of 2-,3- substituted andβ-lactam derivatives of 1,5-benzothiazepine have been synthesized by our team. Furthermore, antimicrobial activities of all these compounds have been researched, and some special structures of these compounds showed high activity. As a continuation of our studies, a series of 3-CH₂CH₂COOCH₃ substituted 1,5-benzothiazepines are synthesized, and on the basis of the 2-substituted 1,5-benzothiazepines, oxadiazole is to be brought in, and fifteen new compounds are synthesized. All the structures of these compounds are determined by IR,¹H NMR and MS, and the antimicrobial activities of all these compounds are tested. At last, the original structure- activity relationship is studied for the foundation of further research.This thesis includes the following parts:Firstly, a series of novel 3-CH₂CH₂COOCH₃ 1,5-benzothiazepines are synthesized by the Friede-Crafts acylation reaction, esterification reaction, Mannich reaction, Michael addition reaction and cyclo- addition reaction, where different substituted benzene is used for the raw materials, and the structures of these new compounds are determined by IR,¹H NMR,MS and X-ray single crystal diffraction method.Secondly, fifteen Oxadiazolo substituted 1,5-benzothiazepine derivatives are synthesized from 2-substituted 1,5-benzothiazepines , and their structures are aslo determined by IR,1H NMR and MS.Lastly, antimicrobial activities of these novel compounds are researched in vitro. And on the foundation of these results, the original structure-activity relationship is studied.