Pleuromutilins. Part 1: The identification of novel mutilin 14-carbamates

Pleuromutilins. Part 1: The identification of novel mutilin 14-carbamates
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DOI:
10.1016/s0968-0896(00)00338-2
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发表时间:
2001-05-01
影响因子:
3.5
通讯作者:
Woodnutt, G
Woodnutt, G
中科院分区:
医学3区
文献类型:
--
作者:
Brooks, G;Burgess, W;Woodnutt, G

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通过对天然抗生素截短侧耳素(1)的结构-活性研究,发现了一系列新的14-氨基甲酸酯。特别是,4-甲氧基苯甲酰基氨基甲酸酯SE-222734(15 o)对许多对目前使用的药剂具有抗性的细菌病原体显示出有效的抗菌活性,并且与早期截短侧耳素衍生物相比,显示出增强的代谢稳定性。因此,此类衍生物具有提供用于人类治疗的新类别的抗细菌剂的潜力,其解决细菌抗性的威胁。(C)2001爱思唯尔科技有限公司版权所有。
A novel series of mutilin 14-carbamates has been discovered as a result of structure-activity studies on the naturally occurring antibiotic pleuromutilin (1). In particular, the 4-methoxybenzoylcarbamate, SE-222734 (15o) displays potent antibacterial activity against a number of bacterial pathogens which are resistant to currently used agents and shows enhanced metabolic stability when compared to earlier pleuromutilin derivatives. Such derivatives therefore have the potential to provide a new class of antibacterial agents for human therapy which address the threat of bacterial resistance. (C) 2001 Elsevier Science Ltd. All rights reserved.