Synthesis and biological evaluation of 6-bromo-6-substituted penicillanic acid derivatives as β-lactamase inhibitors

被引：3
作者：
Bedini, A
Balsamini, C
Di Giacomo, B
Tontini, A
Citterio, B
Giorgi, L
Di Modugno, E
Tarzia, G
机构：
[1] Univ Urbino, Ist Chim Farmaceut, I-61029 Urbino, Italy
[2] Univ Urbino, Ist Sci Tossicol Igienist & Ambientali, I-61029 Urbino, Italy
[3] GlaxoSmithKline Med Res Ctr, I-37135 Verona, Italy
来源：
FARMACO | 2002年 / 57卷 / 08期
关键词：
beta-lactams; beta-lactamase inhibitors; brobactam;
D O I：
10.1016/S0014-827X(02)01261-2
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
The synthesis of a selected set of 6-bromopenicillanic acid derivatives with an additional C6 substituent is reported. All these substances were tested as inhibitors of class A and C beta-lactamase enzymes derived from Escherichia coli (TEM-1) and E. cloacae (P99). As 6-(1-hydroxyethyl) derivatives 4c and 6c were found to be weak beta-lactamase inhibitors, they were further investigated in combination with amoxicillin against a series of beta-lactamase-producing bacterial strains. Some structure-activity relationships are discussed. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.
引用
收藏
页码：663 / 669
页数：7
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