1,5-苯并硫氮杂-α-取代-β-内酰胺衍生物的合成、晶体结构及其抑菌活性

Synthesis,Crystal Structure and Antibacterial Activities of α-Substituted β-lactam Derivatives of 1,5-Benzothiazepines

酰氯与1,5-苯并硫氮杂反应,合成了12个1,5-苯并硫氮杂-α-取代-β-内酰胺衍生物,产物的结构用IR,MS,1H NMR和元素分析表征,立体结构用单晶X-射线衍射法确证。生物活性研究表明,此类化合物有一定的抑菌作用,其中对大肠杆菌的抑菌效果相对较好,但其活性低于1,5-苯并硫氮杂。

Twelve α-substituted β-lactam derivatives of 1,5-benzothiazepine were synthesized and the structures of six as-prepared compounds were confirmed by elemental analysis, IR, MS and ^1H NMR. X-ray analysis revealed that the sevenmember ring in 1,5-benzothiazepines adopts chair-like conformation,two substituents at β-lactam are on the same side, the reaction of 1,5-benzothiazepines with acyl chloride is stereospecific. From the primary biological activity assay it showed that most of twelve products have weak to medium antibacterial activities against S. Aureus, S. Albus, E. Coli, and B. Albicarts, and also showed that their antibacterial activities are lower than 1,5-benzothiazepines .