Pyridazinones as selective cyclooxygenase-2 inhibitors
作者:Chun Sing Li、Christine Brideau、Chi Chung Chan、Chantal Savoie、David Claveau、Stella Charleson、Robert Gordon、Gillian Greig、Jacques Yves Gauthier、Cheuk K Lau、Denis Riendeau、Michel Thérien、Elizabeth Wong、Petpiboon Prasit
DOI:10.1016/s0960-894x(02)01045-4
日期:2003.2
Pyridazinone was found to be an excellent core template for selective COX-2 inhibitors. Two potent. selective and orally active COX-2 inhibitors, which were highly efficacious in rat paw edema and rat paresis models. have been obtained. (C) 2003 Elsevier Science Ltd. All rights reserved.
Synthesis and Antihypertensive Activity of 4-(Diazabicyclo[4.1.0]-heptenyloxy)benzopyran Derivatives and Their Analogues.
0]hept- 2-en-2-yl)oxy]-2H-1-benzopyrans and their analogues were synthesized and evaluated on potassium channel opening and hypotensive activities. Compound (-)-13B with a (4-methyl-5-oxo-3,4-diazabicyclo[4.1.0]hept-2-en-2-yl)oxy group for the 4-position of the benzopyran ring was 3 times as potent as EMD 57283 (II), the lead compound, in hypotensive activity. The results would demonstrate that 5-oxo-3,4-diazabicyclo[4