Anti-Mycobacterium tuberculosis agents derived from quinoxaline-2-carbonitrile and quinoxaline-2-carbonitrile 1,4-di-N-oxide.
In this paper new quinoxaline derivatives with different substituents in positions 3, 6, 7 and 8 are reported. Their biological activities against Mycobacterium tuberculosis have been assessed and most of the 1,4-di-N-oxide derivatives have been shown to strongly inhibit the bacteria growth in the first in vitro screening. One of these N-oxides (4) is a promising candidate due to its good Selectivity Index (7.95). On the other hand, those compounds without N-oxide moieties showed no or very low activity (growth inhibition: 17% and 39%).
Ortega
Miguel Angel
MA
Unidad en Investigación y Desarrollo de Medicamentos, CIFA, Universidad de Navarra, Pamplona, Spain.
Sainz
Yolanda
Y
Montoya
María Elena
ME
Jaso
Andrés
A
Zarranz
Belén
B
Aldana
Ignacio
I
Monge
Antonio
A
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D007202:Indicators and Reagents; D008264:Macrophages / Q000187:drug effects / Q000382:microbiology; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D009570:Nitriles / Q000138:chemical synthesis* / Q000494:pharmacology*; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D014709:Vero Cells
D000970:Antineoplastic Agents; D000995:Antitubercular Agents; D007202:Indicators and Reagents; D009570:Nitriles; D011810:Quinoxalines; C449920:quinoxaline-2-carbonitrile; C449921:quinoxaline-2-carbonitrile 1,4-di-N-oxide