Synthesis and in vitro pharmacology of a series of hybrid molecules possessing 1,4-dihydropyridine calcium-channel blocking activity and histamine H2-agonistic properties

JAM Christiaans*, AD Windhorst, H. van der Goot, H. Timmerman

*Corresponding author for this work

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The synthesis and in vitro pharmacology of a series of new cardiovascular hybrid molecules, which could be useful for the treatment of certain types of hypertension and at the same time for the treatment of cardiac ischemic disease, are discussed. Two types of 1,4-dihydropyridine Ca2+-channel blockers have been studied. In general, hybrid molecules possessing a diethyl 2-(ω-aminoalkylthio)methyl-2,6-dimethyl-4-[(substituted)phenyl]-1,4-dihydropyridine-3,5-dicarboxylic structural moiety and a histamine H2-agonistic structural moiety are more potent L-type calcium-channel blockers and histamine H2-agonists than hybrid molecules containing a diethyl 4-[2-(ω-aminoalkoxy)phenyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic structural moiety.

Original languageEnglish
Pages (from-to)579-593
Number of pages15
JournalEuropean Journal of Medicinal Chemistry
Issue number7-8
Publication statusPublished - 1 Jan 1994

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