A facile synthesis of 1-ethoxy-4-cyano-5-ethoxycarbonyl-3H-azuleno[1,2-c]pyran-3-one, a selective 15-lipoxygenase inhibitor.
A facile method to synthesize 1-ethoxy-4-cyano-5-ethoxycarbonyl-3H-azuleno[1,2-c]pyran-3-one, in yield of 92%, which showed selective inhibition effect on 15-lipoxygenase(soybean source) at IC(50)=24.2+/-2.7 microM while no inhibition effect was observed at greater than 300 microM on 5-lipoxygenase, lipid peroxidase, phospholipase A(2), protein kinase C, and cyclooxygenase.
Lin
Bing Bing
BB
Graduate Institute of Chemistry, Tamkang University, Tamsui, Taipei 251, Taiwan. a332@yahoo.com
Morita
Tadayoshi
T
Lin
Yun-Shan
YS
Chen
Hui-Ling
HL
D000818:Animals; D001093:Arachidonate 15-Lipoxygenase / Q000378:metabolism; D052176:Azulenes; D003508:Cycloheptanes / Q000138:chemical synthesis* / Q000494:pharmacology; D045563:Indolequinones / Q000138:chemical synthesis / Q000494:pharmacology; D016859:Lipoxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D051381:Rats
D052176:Azulenes; D003508:Cycloheptanes; D045563:Indolequinones; D016859:Lipoxygenase Inhibitors; C068040:quinone methide; C005525:azulene; D001093:Arachidonate 15-Lipoxygenase