Synthesis and anti-inflammatory/antioxidant activities of some new ring substituted 3-phenyl-1-(1,4-di-N-oxide quinoxalin-2-yl)-2-propen-1-one derivatives and of their 4,5-dihydro-(1H)-pyrazole analogues.
We report the synthesis, anti-inflammatory and antioxidant activities of novel ring substituted 3-phenyl-1-(1,4-di-N-oxide quinoxalin-2-yl)-2-propen-1-one derivatives and of their 4,5-dihydro-(1H)-pyrazole analogues. The tested compounds inhibit the carrageenin-induced rat paw edema (4.5-56.1%) and present important scavenging activities. Compound 2a is the most potent (56.1%) in the in vivo experiment and exhibits promising in vitro inhibition of soybean lipoxygenase (IC(50)<1microM).
Burguete
Asunción
A
Unidad de Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), Universidad de Navarra, c/Irunlarrea s/n, 31080 Pamplona, Spain.
Pontiki
Eleni
E
Hadjipavlou-Litina
Dimitra
D
Villar
Raquel
R
Vicente
Esther
E
Solano
Beatriz
B
Ancizu
Saioa
S
Pérez-Silanes
Silvia
S
Aldana
Ignacio
I
Monge
Antonio
A
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000627:therapeutic use; D000975:Antioxidants / Q000138:chemical synthesis* / Q000627:therapeutic use; D004487:Edema / Q000188:drug therapy; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000627:therapeutic use; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000627:therapeutic use; D051381:Rats
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000975:Antioxidants; D011720:Pyrazoles; D011810:Quinoxalines