Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 23, Pages 6439-6443Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.10.002
Keywords
quinoxaline 1,4-di-N-oxide; alpha,beta-unsaturated ketone; 4,5-dihydro-(1H)-pyrazole; anti-inflammatory agents; antioxidant agents
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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 (IC50 < 1 mu M). (c) 2007 Elsevier Ltd. All rights reserved.
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