Pyrazinoic acid esters with broad spectrum in vitro antimycobacterial activity

J Med Chem. 1995 Sep 29;38(20):3902-7. doi: 10.1021/jm00020a003.


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.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Esters / pharmacology
  • Microbial Sensitivity Tests
  • Mycobacterium / drug effects*
  • Pyrazinamide / analogs & derivatives*
  • Pyrazinamide / pharmacology
  • Structure-Activity Relationship


  • Anti-Bacterial Agents
  • Esters
  • Pyrazinamide
  • pyrazinoic acid