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Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Brain EG,Eglington AJ,James BG,Nayler JH,Osborne NF,Pearson MJ,Smale TC,Southgate R,Tolliday P,Basker MJ,Mizen LW,Sutherland R

doi

10.1021/jm00218a019

subject

Has Abstract

pub_date

1977-08-01 00:00:00

pages

1086-90

issue

8

eissn

0022-2623

issn

1520-4804

journal_volume

20

pub_type

杂志文章

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