Studies On The Synthesis And Antimicrobial Activities Of 1 ,5-Benzothiazepines Containning The Heterocycles

1,5 - benzothiazepine is a kind of seven-membered heterocyclic compound which has important physiological activities.Some of their derivatives have been used in clinic as antianxiety drugs,hypnogenetics and cardiovascular medicines. Furan,thiophene,oxadiazole and other heterocycles are a class of compounds with various bioactivities, some of which can be used as drugs, pesticides, herbicides, dyes, etc.Some of their derivatives in medicine, pesticide and other fields also have a wide range of application. Therefore, 1,5-benzothiazepine and heterocyclic compounds'structure,syntheses and pharmacological activities alaways attract wide attention of human beings.There has long been engaged in the synthesis of 1,5 - benzothiazepine derivatives and the research of their antimicrobial activities in our laboratory, and 2-and 3- ester substitutd in the seven-membered derivatives of 1,5– benzothiazepine have been synthesized. Test results of the antimicrobial activity show that some of these compounds have good antimicrobial effects on bacteria and fungi, which will have important significance to find the new physiological activity's and special function's drugs. On this basis, in view of furan, thiophene,oxadiazole and other heterocyclic compounds with some antimicrobial activity, 2–Furan,thiophene and other heterocycles and 3-ester substitutd 1,5-benzothiazepines are synthesized and some of these compounds are structurally modified.The antimicrobial activities of the compounds synthesized are tested in order to obtain better antimicrobial activity's compounds.The main job in this thesis is as follows:Firstly, a series of 1,5 - benzothiazepines containing furan and thiophene rings are synthesized by reaction steps, where ethyl acetoacetate and furan,thiophene and other heterocyclic aldehyde are used for the raw materials,and the structures of these new compounds are determined by IR,1H NMR,MS,elemental analysis and X-ray single crystal diffraction method.Secondly, 1,5-benzothiazepines containing 1,2,4-oxadiazole rings are synthesized through a series of reactions and their structures are determined by IR,1H NMR,MS and elemental analysis . Thirdly, 5 products are synthesized by the reduction of the imine double bond and their structures are determined by IR,1H NMR,MS and elemental analysis.Lastly, antimicrobial activities of 27 novel compounds are researched in vitro. And on the foundation of these results, the original structure-activity relationship is studied.