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 r...

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Veröffentlicht in:	Journal of medicinal chemistry 2002-12, Vol.45 (25), p.5604-5606
Hauptverfasser:	Seitz, Lainne E, Suling, William J, Reynolds, Robert C
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Medical sciences Microbial Sensitivity Tests Mycobacterium avium - drug effects Mycobacterium tuberculosis - drug effects Pharmacology. Drug treatments Pyrazinamide - analogs & derivatives Pyrazinamide - chemical synthesis Pyrazinamide - chemistry Pyrazinamide - pharmacology Pyrazines - chemical synthesis Pyrazines - chemistry Pyrazines - pharmacology Quinoxalines - chemical synthesis Quinoxalines - chemistry Quinoxalines - pharmacology Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	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 μg/mL) but only modest activity against MAC (MICs of 4−32 μg/mL).
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm020310n