Brain E G, Eglington A J, James B G, Nayler J H, Osborne N F, Pearson M J, Smale T C, Southgate R, Tolliday P, Basker M J, Mizen L W, Sutherland R
J Med Chem. 1977 Aug;20(8):1086-90. doi: 10.1021/jm00218a019.
A previously outlined general procedure for preparing various 3-substituted cephalosporins from the penicillin nucleus has been used, with modifications where required, to prepare a series of analogues of cephalexin with various substituents in the 3-methyl group. The 3-substituents most conducive to broad-spectrum antibacterial activity were 3-pyridylmethyl and m- or p-carboxybenzyl. The compounds were only poorly absorbed by the oral route in mice, but the 3-(carboxybenzyl) compounds gave more prolonged useful serum levels than the usual cephalosporins.
一种先前概述的从青霉素核制备各种3-取代头孢菌素的通用方法已被使用，并在需要时进行了修改，以制备一系列在3-甲基上带有各种取代基的头孢氨苄类似物。最有利于广谱抗菌活性的3-取代基是3-吡啶基甲基和间位或对位羧基苄基。这些化合物经小鼠口服后吸收很差，但3-(羧基苄基)化合物比常用的头孢菌素能提供更长时间的有效血清水平。
