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PH-027与利奈唑胺及其他抗厌氧菌抗菌药物对艰难梭菌及其他厌氧菌临床分离株的体外活性比较

Comparative in vitro activity of PH-027 versus linezolid and other anti-anaerobic antimicrobials against clinical isolates of Clostridium difficile and other anaerobic bacteria.

作者信息

Phillips O A, Rotimi V O, Jamal W Y, Shahin M, Verghese T L

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kuwait University, Safat, Kuwait.

出版信息

J Chemother. 2003 Apr;15(2):113-7. doi: 10.1179/joc.2003.15.2.113.

Abstract

PH-027 is a new 5-triazole oxazolidinone synthesized in our laboratories, which shows strong activity against gram-positive aerobic bacteria including clinical isolates. The objective of this study was to investigate the in vitro activity of this compound in comparison with linezolid and other antibiotics against gram-positive and gram-negative anaerobes. The in vitro activity of PH-027 in comparison with those of linezolid and other antimicrobial agents was evaluated against 201 clinical isolates of gram-positive and gram-negative anaerobic bacteria by agar dilution and Etest methods. PH-027 showed excellent activity, with minimum inhibitory concentrations (MIC) in the range of 0.12-4.0 microg/ml against all isolates; MIC90s being 4.0, 1.0, 2.0, 2.0 and 2.0 microg/ml against Clostridium difficile, Peptostreptococcus spp., Bacteroides fragilis, Prevotella bivia and Fusobacterium spp. respectively. In comparison, linezolid had MIC in the range of 0.5-4.0 microg/ml against all isolates, with MIC90s of 2.0, 4.0, 4.0, 4.0 and 2.0 microg/ml against the same set of bacteria respectively. PH-027 demonstrated excellent in vitro activity that is superior to linezolid against Peptostreptococcus spp., B. fragilis and P. bivia. However, against C. difficile and Fusobacterium spp, PH-027 and linezolid showed comparable in vitro activity. Against all anaerobes, metronidazole, PH-027 and, to a lesser extent, linezolid had the most potent activity. From the results of in vitro susceptibility testing, both linezolid and PH-027 show promise in the treatment of anaerobic infections.

摘要

PH - 027是我们实验室合成的一种新型5 - 三唑恶唑烷酮,对包括临床分离株在内的革兰氏阳性需氧菌显示出强大活性。本研究的目的是将该化合物与利奈唑胺及其他抗生素进行比较,研究其对革兰氏阳性和革兰氏阴性厌氧菌的体外活性。通过琼脂稀释法和Etest法,对201株革兰氏阳性和革兰氏阴性厌氧菌临床分离株评估了PH - 027与利奈唑胺及其他抗菌剂的体外活性。PH - 027表现出优异的活性,对所有分离株的最低抑菌浓度(MIC)在0.12 - 4.0微克/毫升范围内;对艰难梭菌、消化链球菌属、脆弱拟杆菌、二路普雷沃菌和梭杆菌属的MIC90分别为4.0、1.0、2.0、2.0和2.0微克/毫升。相比之下,利奈唑胺对所有分离株的MIC在0.5 - 4.0微克/毫升范围内,对同一组细菌的MIC90分别为2.0、4.0、4.0、4.0和2.0微克/毫升。PH - 027表现出优异的体外活性,在抗消化链球菌属、脆弱拟杆菌和二路普雷沃菌方面优于利奈唑胺。然而,在抗艰难梭菌和梭杆菌属方面,PH - 027和利奈唑胺表现出相当的体外活性。对所有厌氧菌而言,甲硝唑、PH - 027以及在较小程度上利奈唑胺具有最强的活性。从体外药敏试验结果来看,利奈唑胺和PH - 027在治疗厌氧菌感染方面都有前景。

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