Synthesis and in Vitro and in Vivo Characteristics of an Iodinated Analogue of the β-Adrenoceptor Antagonist Carazolol

EA Dubois, JC van den Bos, T Doornbos…

Index: Dubois, Eric A.; Van Den Bos, Jan C.; Doornbos, Tamme; Van Doremalen, Peter A. P. M.; Somsen, G. Aernout; Vekemans, Jozef A. J. M.; Janssen, Anton G. M.; Batink, Harry D.; Boer, Gerard J.; Pfaffendorf, Martin; Van Royen, Eric A.; Van Zwieten, Pieter A. Journal of Medicinal Chemistry, 1996 , vol. 39, # 17 p. 3256 - 3262

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Citation Number: 26

Abstract

A new (radio) iodinated, β-adrenoceptor ligand,(S)-(-)-4-[3-[(1, 1-dimethyl-3-iodo-(2 E)- propenyl) amino]-2-hydroxypropoxy] carbazole (CYBL8E, 1), was prepared. 1 is an iodinated analogue of the high-affinity β-adrenoceptor antagonist carazolol (2). The asymmetric synthesis was achieved in four steps starting from 4-hydroxycarbazole. The iodine-123-labeled form was obtained by an iododestannylation reaction with [123I] NaI in ...