一系列吡嗪酸酯的抗分枝杆菌活性

Antimycobacterial activity of a series of pyrazinoic acid esters.

作者信息

Cynamon M H, Klemens S P, Chou T S, Gimi R H, Welch J T

机构信息

Department of Medicine, VA Medical Center, Syracuse, New York.

出版信息

J Med Chem. 1992 Apr 3;35(7):1212-5. doi: 10.1021/jm00085a007.

DOI:10.1021/jm00085a007

PMID:1560435

Abstract

A series of pyrazinoic acid esters has been prepared and evaluated for in vitro antimycobacterial activity. Several of the pyrazinoate esters have substantially better activity than the first-line antituberculous agent pyrazinamide against susceptible isolates of Mycobacterium turberculosis as well as activity against pyrazinamide-resistant isolates. The minimal inhibitory concentrations (MICs) were lower for each organism and at each pH than the MICs for pyrazinamide. The esters have activity against Mycobacterium bovis and Mycobacterium kansasii, two species resistant to pyrazinamide, but not against Mycobacterium avium complex.

摘要

已制备了一系列吡嗪酸酯，并对其体外抗分枝杆菌活性进行了评估。几种吡嗪酸酯对结核分枝杆菌敏感菌株的活性明显优于一线抗结核药物吡嗪酰胺，并且对吡嗪酰胺耐药菌株也有活性。每种菌株在各pH值下的最低抑菌浓度（MIC）均低于吡嗪酰胺的MIC。这些酯对牛分枝杆菌和堪萨斯分枝杆菌（两种对吡嗪酰胺耐药的菌种）有活性，但对鸟分枝杆菌复合群无活性。