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自1981年发现了具有抗菌活性的单环β-内酰胺抗生素以来,人们对此产生了广泛的兴趣。该类抗生素不仅对各种β-内酰胺酶较为稳定,而且对革蓝氏阴性菌有较强的抗菌活性。并且结构简单,可用全合成的方法制备各种不同侧链的衍生物,见图1。有关化学合成、生物学特性及构效关系已有许多综述性文章报道。以氨基酸为原料,合成单环刀—内酰胺母核的方法也介绍了不少。但全合成具有抗菌活性的单酰胺菌素尚未见有报道。
Since 1981, antibacterial activity has been found monocyclic β-lactam antibiotics, this has been a widespread interest. Such antibiotics not only for a variety of β-lactamase more stable, but also against Gram-negative bacteria have strong antibacterial activity. And the structure is simple, all synthetic methods can be used to prepare a variety of different side chain derivatives, shown in Figure 1. There are many comprehensive articles on chemical synthesis, biological properties and structure-activity relationship. Amino acids as raw materials, synthetic monocycle knife - lactam mother nucleus also introduced a lot. However, the synthesis of antibacterial activity of monobactam has not been reported.