Structure-activity relationship in the oxazolidinone-quinolone hybrid series: Influence of the central spacer on the antibacterial activity and the mode of action
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: Influence of the central spacer on the antibacterial activity and the mode of action
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DOI：
10.1016/j.bmcl.2003.07.028
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发表时间：
2003-12-01
影响因子：
2.7
通讯作者：
Locher, HH
中科院分区：
文献类型：
--
作者：
Hubschwerlen, C;Specklin, JL;Locher, HH
合成了联合收割机喹诺酮和恶唑烷酮药效团的恶唑烷酮-喹诺酮杂合物，并显示其对多种敏感和耐药革兰氏阳性和革兰氏阴性细菌具有活性。间隔基的性质通过指导作用模式（即醌和/或恶唑烷酮样活性）极大地影响抗菌活性。该系列中的最佳化合物具有平衡的双重作用模式，并克服临床相关革兰氏阳性病原体中的所有类型的耐药性，包括对喹诺酮类和利奈唑胺的耐药性。(C)2003爱思唯尔有限公司。保留所有权利。
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.