半合成头孢菌素。III. 新型口服活性7-[4-羟基-3-(取代甲基)苯基]-乙酰胺基-3-头孢烯-4-羧酸的合成及构效关系
Semisynthetic cephalosporins. III. Synthesis and structure activity relationships of novel orally active 7-[4-hydroxy-3-(substituted methyl)phenyl]-acetamido-3-cephem-4-carboxylic acids.
作者信息
Nudelman A, Patchornick A, Karoly-Hafely E, Braun F, Erickson R C
出版信息
J Antibiot (Tokyo). 1980 Jan;33(1):76-82. doi: 10.7164/antibiotics.33.76.
PMID:7372553
Abstract
A family of novel optically active alpha-amino-3-substituted-methyl-4-hydroxy benzene acetic acids (3) have been prepared. A number of these amino acids were converted to a group of cephalosporins (12). Compound 12A showed the most interesting activity in vitro and in vivo, primarily against Gram-positive organisms and was shown to be well absorbed orally.
摘要
已制备出一类新型旋光性α-氨基-3-取代甲基-4-羟基苯乙酸（3）。其中一些氨基酸被转化为一组头孢菌素（12）。化合物12A在体外和体内均表现出最有趣的活性，主要针对革兰氏阳性菌，且显示口服吸收良好。
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