Electrophilic derivatives of purines as irreversible inhibitors of A1 adenosine receptors

KA Jacobson, S Barone, U Kammula…

Index: Jacobson; Barone; Kammula; Stiles Journal of Medicinal Chemistry, 1989 , vol. 32, # 5 p. 1043 - 1051

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Citation Number: 46

Abstract

Functionalized congeners derived from 1, 3-dipropyl-8-phenylxanthine and from p- phenyladenosine were derivatized to contain electrophilic groups (isothiocyanate, N- hydroxysuccinimide ester, maleimide, sulfonyl chloride, or a-haloacyl group) capable of reaction with nucleophiles on biopolymers. The goal was to inhibit chemically the AI adenosine receptor by using reactive agonist and antagonist ligands. Some of the ...