Structure-activity relationship in the oxazolidinone-quinolone hybrid series: Influence of the central spacer on the antibacterial activity and the mode of action

被引：50

作者：

Hubschwerlen, C ^{[1
]}

Specklin, JL ^{[1
]}

Baeschlin, DK ^{[1
]}

Borer, Y ^{[1
]}

Haefeli, S ^{[1
]}

Sigwalt, C ^{[1
]}

Schroeder, S ^{[1
]}

Locher, HH ^{[1
]}

机构：

[1] Morphochem AG, CH-4058 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 23期

关键词：

D O I：

10.1016/j.bmcl.2003.07.028

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Oxazolidinone-quinolone hybrids, which combine the pharmacophores of a quinolone and an oxazolidinone, were synthesised and shown to be active against a variety of susceptible and resistant Gram-positive and Gram-negative bacteria. The nature of the spacer greatly influences the antibacterial activity by directing the mode of action, that is quinotone- and/or oxazolidinone-like activity. The best compounds in this series have a balanced dual mode of action and overcome all types of resistance, including resistance to quinolones and linezolid, in clinically relevant Gram-positive pathogens. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：4229 / 4233

页数：5

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