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。I. 7β-[2-烷基-和2-羟基-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. I. Synthesis and antibacterial activity of 7 beta-[2-alkyl- and 2-hydroxy-2-(2-aminothiazol-4-yl)-acetamido]cephalosporins.
作者信息
Ochiai M, Morimoto A, Matsushita Y, Kaneko T, Kida M
出版信息
J Antibiot (Tokyo). 1980 Sep;33(9):1005-13. doi: 10.7164/antibiotics.33.1005.
PMID:7440407
Abstract
2-Alkyl- and 2-hydroxy derivatives of 7 beta-[2-aminothiazol-4-yl)acetamido]cephalosporins were synthesized to improve the antibacterial activity of the parent compounds especially against beta-lactamase-producing organisms. Some of these compounds showed an increase in activity against Serratia marcescens (Xb, XXIIIa) and Enterobacter cloacae (Xb, XIV). The 2,2-dimethyl derivative (XXVIIIb) showed a definite loss of activity.
摘要
合成了7β-[（2-氨基噻唑-4-基）乙酰胺基]头孢菌素的2-烷基和2-羟基衍生物，以提高母体化合物的抗菌活性，特别是对产生β-内酰胺酶的微生物的抗菌活性。其中一些化合物对粘质沙雷氏菌（Xb，XXIIIa）和阴沟肠杆菌（Xb，XIV）的活性有所增加。2,2-二甲基衍生物（XXVIIIb）的活性明显丧失。
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