Conformational requirements for histamine H2-receptor inhibitors: a structure-activity study of phenylene analogs related to cimetidine and tiotidine

…, ML Torchiana, WC Lumma Jr, JJ Baldwin

Index: Hoffman; Pietruszkiewicz; Habecker; Phillips; Bolhofer; Cragoe Jr.; Torchiana; Lumma Jr.; Baldwin Journal of Medicinal Chemistry, 1983 , vol. 26, # 2 p. 140 - 144

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Citation Number: 22

Abstract

Two series of compounds related to cimetidine and tiotidine were synthesized as part of a study to evaluate the importance of conformational parameters in binding at histamine Hz receptors. The flexible methylthioethyl connecting chain was replaced by a conformationally restricting phenylene unit. These compounds were evaluated for antagonism of the dimaprit- stimulated chronotropic response in the guinea pig atrium and inhibition of histamine ...