Synthesis and antibacterial activity of dual-action agents of a β-lactam antibiotic with cytotoxic agent mitozolomide or temozolomide

被引:19
作者
Wang, YF [1 ]
Lambert, P [1 ]
Zhao, LX [1 ]
Wang, D [1 ]
机构
[1] Aston Univ, Pharmaceut Res Inst, Birmingham B4 7ET, W Midlands, England
关键词
dual-action; antibacterial; beta-lactam; cytotoxic; tetrazinone;
D O I
10.1016/S0223-5234(01)01331-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Dual-action agents 5a-f and 12a-f. a beta-lactam antibiotic combined with a cytotoxic agent. mitozolomide (Meto) or temozolomide (Temo). were synthesised. The antibacterial activity (MICs) of the dual-action agents has been determined against a panel of bacteria including several beta-lactamase producing strains. The tests showed 5a-f active against the non-p-lactamase producing methicillin sensitive Staphylococcus aureus (MSSA) strains. however, little synergistic effect between the P-lactam and the cytotoxic agent was observed. 12a-f demonstrated some synergistic effect against bacteria. 12a. in particular. is active against ampicillin resistant (beta-lactamase-producing) strains of Serratia marcescens. (C) 2002 Published by editions scientifiques et medicales Elsevier SAS.
引用
收藏
页码:323 / 332
页数:10
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