Synthesis and antimycobacterial activity of pyrazine and quinoxaline derivatives.
A series of pyrazine and quinoxaline derivatives have been synthesized, and their activity against M. tuberculosis (Mtb) and Mycobacterium avium (MAC) are reported. The 4-acetoxybenzyl ester of pyrazinoic acid and 4'-acetoxybenzyl 2-quinoxalinecarboxylate showed excellent activity against Mtb (MIC ranges of less than 1-6.25 microg/mL) but only modest activity against MAC (MICs of 4-32 microg/mL).
Seitz
Lainne E
LE
Organic Chemistry Department, Southern Research Institute, P.O. Box 55305, Birmingham, Alabama 35255-5305, USA.
Suling
William J
WJ
Reynolds
Robert C
RC
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009162:Mycobacterium avium / Q000187:drug effects*; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011718:Pyrazinamide / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011719:Pyrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
C469915:4'-acetoxybenzyl 2-quinoxalinecarboxylate; C469914:4-acetoxybenzyl pyrazinoate; D000900:Anti-Bacterial Agents; D011719:Pyrazines; D011810:Quinoxalines; D011718:Pyrazinamide