Irreversible H2-antagonism of the four isomeric butyl analogues of mifentidine |
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Authors: | H. M. M. Bastiaans A. Donetti K. Kramer G. Bietti E. Cereda D. Dubini M. Mondini A. Bast H. Timmerman |
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Affiliation: | (1) Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands;(2) Research Laboratories of Instituto De Angeli, Via Serio 15, I-20139 Milan, Italy |
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Abstract: | It has been hypothesized that bidentate hydrogen bonding plays an important role in the interaction of imidazolylphenylformamidines with the H2-receptor. The present study, in which the degree of pseudoirreversible H2-antagonism of the four isomeric butyl substituted mifentidine analogues was determined on the spontaneously beating right atrium of the male guinea-pig, lends further support to this hypothesis. In solution the EE/EZ ratio is different for the four isomeric butylated mifentidine analogues. The rank order of the percentage of E,E conformation, which favors a bidentate interaction, of the formamidine moiety parallels the rank order of pseudo-irreversible H2-antagonism. |
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