Antimycobacterial activity of a series of pyrazinoic acid esters.
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.
Cynamon
M H
MH
Department of Medicine, VA Medical Center, Syracuse, New York.
Klemens
S P
SP
Chou
T S
TS
Gimi
R H
RH
Welch
J T
JT
D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000494:pharmacology; D004952:Esters / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D006863:Hydrogen-Ion Concentration; D051379:Mice; D009161:Mycobacterium / Q000187:drug effects*; D009162:Mycobacterium avium / Q000187:drug effects; D009163:Mycobacterium bovis / Q000187:drug effects; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D011718:Pyrazinamide / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity
D000995:Antitubercular Agents; D004952:Esters; D011718:Pyrazinamide; C005296:pyrazinoic acid