11个单环β-内酰胺类化合物的合成及其抗菌活性初探

Synthesis of 11 monobactams and their antibacterial activity

根据单环 β-内酰胺类化合物定量构效关系研究的结果提示 ,以 N-苄基 - 3(S) -邻苯二甲酰亚胺基- 4 (S) - [4 (S) - 2 ,2 -二甲基 - 1,3二氧环戊 - 4 -基 ]- 2 -氧吖丁啶为原料 ,设计合成了 11个新的单环 β-内酰胺类化合物 ,其结构经 MS、1 H- NMR或 IR所确证 ,并测定了它们的体外抗菌活性 ,结果表明 ,它们均有抗菌作用 ,但抗菌活性低于对照品。

Based on the result of quantitative structure activity relationship (QSAR) which was studied among monobactams, 11 new monobactams were designed and synthesized from N-benzyl-3(S)-phthalimido-4(S)-[4(S)-2,2-dimethyl-1,3-dioxolan-4-yl]-2-oxo-azetidine, their structure had been determined by 1H-NMR or IR and MS, and in vitroantibacterial activities of these compounds were tested. Results showed that they have lower activities than those of control compounds.