Document Report Card

ID: ALA1123905

Journal: J Med Chem

Title: Zwitterionic analogues of cimetidine as H2 receptor antagonists.

Authors: Young RC, Ganellin CR, Graham MJ, Mitchell RC, Roantree ML, Tashma Z.

Abstract: A series of analogues of the H2 receptor histamine antagonist cimetidine have been synthesized in which the dipolar cyanoguanidine group has been replaced by a number of zwitterionic moieties. Although none of the compounds is more effective than cimetidine in blocking histamine-stimulated tachycardia on the isolated guinea pig atrium, the activities of most of the compounds possessing rigid dipoles can be accounted for on the basis of dipole orientation relative to the common side chain and by considering the active species in each case to be the zwitterion. These findings are in general agreement with those found for analogues having conjugated groups as dipoles.

CiteXplore: 2885416

DOI: 10.1021/jm00390a006