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硫霉素Thienamycin(1)对革兰氏阳性菌及革兰氏阴性菌有很强的抗菌作用(对假单孢菌的抗菌作用特别有意义)。同时对分解β-内酰胺的β-内酰胺酶有耐性,硫霉素在结构上与有代表性的β-内酰胺抗生素的青霉素、头孢菌素不同,分子中不含有硫原子,而且β-内酰胺环的二个氢原子有转移的关系。最近随着硫霉素的全合成,默克公司的研究室发表了有关若干同系物的合成及其抗菌作用的报告。Shih等将硫霉素的氨基乙硫基的氢取代得到脱半胱氨硫霉素(2),研究它是否
Thienamycin (1) has a strong antibacterial activity against Gram-positive and Gram-negative bacteria (of particular interest for the antibacterial effect of Pseudomonas). At the same time on the decomposition of β-lactamase β-lactamase resistant, thiophanin in the structure and the representative β-lactam antibiotics penicillin, cephalosporin, the molecule does not contain sulfur atoms, and β- The two hydrogen atoms of the lactam ring have a metastatic relationship. Recently, with the complete synthesis of thiophanmycin, Merck’s laboratory published reports on the synthesis and antibacterial activity of several homologues. Shih et al. Substituted the hydrogen of aminoethylthiocarbothiolate of thiamycin to give cysteicamycin (2) and investigated whether it is