PYRAZINOIC ACID-ESTERS WITH BROAD-SPECTRUM IN-VITRO ANTIMYCOBACTERIAL ACTIVITY

被引：73

作者：

CYNAMON, MH

GIMI, R

GYENES, F

SHARPE, CA

BERGMANN, KE

HAN, HJ

GREGOR, LB

RAPOLU, R

LUCIANO, G

WELCH, JT

机构：

[1] SUNY HLTH SCI CTR,SYRACUSE,NY 13210

[2] SUNY ALBANY,DEPT CHEM,ALBANY,NY 12222

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 38卷 / 20期

关键词：

D O I：

10.1021/jm00020a003

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of substituted pyrazinoic acid esters has been prepared and examined for their in vitro activity against Mycobacterium avium and Mycobacterium Kansasii as well as Mycobacterium tuberculosis. Modification of both the pyrazine nucleus and the ester functionality have been very successful in expanding the activity of pyrazinamide to include M. avium and M. kansasii, organisms normally not susceptible to pyrazinamide. Several of these compounds have activities 100-1000-fold greater than that of pyrazinamide against M. tuberculosis.

引用

页码：3902 / 3907

页数：6

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