Design, synthesis and biological evaluation of oxazolidinone-quinolone hybrids

被引：74

作者：

Hubschwerlen, C ^{[1
]}

Specklin, JL ^{[1
]}

Sigwalt, C ^{[1
]}

Schroeder, S ^{[1
]}

Locher, HH ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 10期

关键词：

D O I：

10.1016/S0968-0896(03)00083-X

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Oxazolidinone-quinolone hybrids that combine the pharmacophores of a quinolone and an oxazolidinone were synthesised and shown to be active against a variety of resistant and susceptible Gram-positive and fastidious Gram-negative organisms. The best compounds in this series overcome all types of resistance in relevant clinical Gram-positive pathogens. The nature of the spacer greatly influences the antibacterial activity. The dual mode of action could be demonstrated for compounds having a piperazinyl spacer. Antibacterial activity was higher at acidic pH. (C) 2003 Elsevier Science Ltd. All rights reserved.

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页码：2313 / 2319

页数：7

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