Alkylating prazosin analog: irreversible label for. alpha. 1-adrenoceptors

…, Z Szurmai, W Buchowiecki, JW Kusiak

Index: Pitha, Josef; Szabo, Lajos; Szurmai, Zoltan; Buchowiecki, Wieslaw; Kusiak, John W. Journal of Medicinal Chemistry, 1989 , vol. 32, # 1 p. 96 - 100

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Citation Number: 15

Abstract

A series of prazosin analogues comprised of N-acyl derivatives of N'-(4-amino-6, 7- dimethoxyquinazolin-2-yl) piperazine was prepared and the nature of their binding to a,- adrenoceptors was investigated. Derivatives with a,@-unsaturated acyclic acyls had some affinity but no irreversible action at the receptor. Other potent compounds, also without irreversible activity, contained cinnamoyl or (pheny1amino) thiocarbonyl residues. High ...