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新型恶唑烷酮类化合物OCID0050的体外抗菌活性

In vitro antibacterial activities of a novel oxazolidinone, OCID0050.

作者信息

Paul-Satyaseela Maneesh, Solanki Shakti Singh, Sathishkumar Devarajan, Bharani Thirunavukkarasu, Magesh Vijayan, Rajagopal Sriram

机构信息

Anti-infectives Discovery, Department of Microbiology, Orchid Research Laboratories Ltd, 476/14, OMR, Sholinganallur, Chennai 600 119 (TN), India.

出版信息

J Antimicrob Chemother. 2009 Oct;64(4):797-800. doi: 10.1093/jac/dkp300. Epub 2009 Aug 18.

Abstract

OBJECTIVES

In the pursuit of developing a second-generation oxazolidinone, we have identified OCID0050 as a novel oxazolidinone with enhanced activity against bacterial strains resistant to methicillin, vancomycin and linezolid.

METHODS

MIC and MBC determinations were performed according to CLSI guidelines. Linezolid-resistant bacterial strains were generated in-house; inoculum effect, pH effect and kill kinetics experiments were performed as per standard protocols.

RESULTS AND CONCLUSIONS

OCID0050 demonstrated better inhibitory potency against many of the tested clinically significant strains by generally showing 2-4-fold lower MICs than linezolid. In addition, it has higher inhibitory activity against linezolid-resistant strains.

摘要

目的

在开发第二代恶唑烷酮的过程中,我们确定OCID0050是一种新型恶唑烷酮,对耐甲氧西林、万古霉素和利奈唑胺的细菌菌株具有增强的活性。

方法

根据CLSI指南进行最低抑菌浓度(MIC)和最低杀菌浓度(MBC)测定。利奈唑胺耐药细菌菌株在内部产生;按照标准方案进行接种物效应、pH效应和杀菌动力学实验。

结果与结论

OCID0050对许多测试的临床重要菌株表现出更好的抑制效力,其MIC通常比利奈唑胺低2至4倍。此外,它对利奈唑胺耐药菌株具有更高的抑制活性。

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