PYRAZINOIC ACID-ESTERS WITH BROAD-SPECTRUM IN-VITRO ANTIMYCOBACTERIALACTIVITY

Authors
CYNAMON MH GIMI R GYENES F SHARPE CA BERGMANN KE HAN HJ GREGOR LB RAPOLU R LUCIANO G WELCH JT
Citation
Mh. Cynamon et al., PYRAZINOIC ACID-ESTERS WITH BROAD-SPECTRUM IN-VITRO ANTIMYCOBACTERIALACTIVITY, Journal of medicinal chemistry, 38(20), 1995, pp. 3902-3907
Citations number
17
Categorie Soggetti
Chemistry Medicinal
Journal title
Journal of medicinal chemistry → ACNP
ISSN journal
00222623
Volume
38
Issue
20
Year of publication
1995
Pages
3902 - 3907
Database
ISI
SICI code
0022-2623(1995)38:20<3902:PAWBIA>2.0.ZU;2-Y
Abstract
A series of substituted pyrazinoic acid esters has been prepared and e xamined for their in vitro activity against Mycobacterium avium and My cobacterium Kansasii as well as Mycobacterium tuberculosis. Modificati on 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 pyrazin amide. Several of these compounds have activities 100-1000-fold greate r than that of pyrazinamide against M. tuberculosis.