Synthesis and Biological Activities of Flavonoid Derivatives as A<sub>3</sub> Adenosine Receptor Antagonists
作者:Yishai Karton、Ji-long Jiang、Xiao-duo Ji、Neli Melman、Mark E. Olah、Gary L. Stiles、Kenneth A. Jacobson
DOI:10.1021/jm950923i
日期:1996.1.1
vs rat A1 or A2A receptors. The 2-styryl-6-propoxy derivative, 20, of the furanochromone visnagin was 30-fold selective for human A3 receptors vs either rat A1 or A2A receptors. Several of the more potentderivatives effectively antagonized the effects of an agonist in a functional A3 receptor assay, i.e. inhibition of adenylyl cyclase in CHO cells expressing cloned rat A3 receptors. In conclusion,
A compound of the formula (I) ##STR1## in which: R.sub.1 represents a hydrogen atom, a lower alkyl group, a hydroxy group or a lower alkoxy group, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.11 are as defined in the description. Medicaments.