7β-[2-(2-氨基噻唑-4-基)乙酰胺基]头孢菌素衍生物的合成及其构效关系。III. 7β-[2-氨基-2-(2-氨基噻唑-4-基)乙酰胺基]头孢菌素的合成与抗菌活性
Synthesis and structure-activity relationships of 7 beta-[2-(2-aminothiazol-4-yl)acetamido]-cephalosporin derivatives. III. Synthesis and antibacterial activity of 7 beta-[2-amino-2-(2-aminothiazol-4-yl)acetamido]cephalosporins.
作者信息
Ochiai M, Morimoto A, Okada T, Matsushita Y, Yamamoto H, Aki O, Kida M
出版信息
J Antibiot (Tokyo). 1980 Sep;33(9):1022-30. doi: 10.7164/antibiotics.33.1022.
PMID:7440409
Abstract
New derivatives of 7 beta-[2-(2-aminothiazol-4-yl)acetamido]cephalosporins having amino group at the 2-position of the 7-acyl moiety were synthesized in the hope that they would show improved antibacterial activity. Some of these compounds (XXa, XXd, XVb) showed improved activity against Enterobacter cloacae. Replacement of the annular amino group by a methyl group caused loss of activity.
摘要
合成了7β-[2-(2-氨基噻唑-4-基)乙酰胺基]头孢菌素的新衍生物，其在7-酰基部分的2-位上具有氨基，希望它们能表现出改善的抗菌活性。其中一些化合物（XXa、XXd、XVb）对阴沟肠杆菌显示出改善的活性。用甲基取代环状氨基导致活性丧失。
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