CEPHALOSPORINS HAVING A HETEROCYCLIC CATECHOL IN THE C3 SIDE-CHAIN .1. ENHANCEMENT OF EFFICACY AGAINST GRAM-NEGATIVE BACTERIA

被引：9

作者：

IMAE, K ^{[1
]}

HASEGAWA, T ^{[1
]}

OKITA, T ^{[1
]}

HIRANO, M ^{[1
]}

KAMACHI, H ^{[1
]}

KAMEI, H ^{[1
]}

机构：

[1] BRISTOL MYERS SQUIBB KK,BRISTOL MYERS SQUIBB RES INST,MEGURO KU,TOKYO 153,JAPAN

来源：

JOURNAL OF ANTIBIOTICS | 1993年 / 46卷 / 05期

关键词：

D O I：

10.7164/antibiotics.46.840

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Two groups of cephalosporins substituted with a variety of heterocyclic catechols in the C3 side chain were synthesized. One is a group of 3-(heterocyclic catechol-substituted methyl)cephalosporins and another is 3-[(E)-3-heterocyclic catechol-substituted 1-propen-1-yl]cephalosporins. Cephalosporins in the latter group showed higher in vivo efficacies than those in the former group having the same heterocyclic catechol, especially against Pseudomonas aeruginosa A9843A, although there was no significant difference between their in vitro activity. Among the latter group, the 5,6-dihydroxybenzimidazole derivative (6e) and the 2,6-dihydro-7-hydroxy-6-oxo-isoquinoline derivative (6b) showed much higher activity than ceftazidime (CAZ) and imipenem (IPM) against P. aeruginosa A9843A both in in vitro and in vivo studies.

引用

页码：840 / 849

页数：10

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