Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists

…, C Gallo-Rodriguez, N Melman, B Fischer…

Index: Jacobson; Gallo-Rodriguez; Melman; Fischer; Maillard; Van Bergen; Van Galen; Karton Journal of Medicinal Chemistry, 1993 , vol. 36, # 10 p. 1333 - 1342

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Citation Number: 154

Abstract

A series of substituted 8-styryl derivatives of 1, 3, 7-alkylxanthines was synthesized as potential Az-selective adenosine receptor antagonists, and the potency at rat brain AI-and Az-receptors was studied in radioligand binding experiments. At the xanthine 7-position, only small hydrophobic substituents were tolerated in receptor binding. 7-Methyl analogues were roughly 1 order of magnitude more selective for A2 versus Al receptors than the ...