Collect. Czech. Chem. Commun. 1992, 57, 169-178

Synthesis and Calcium Antagonist Activity of Dialkyl 1,4-Dihydro-2,6-dimethyl-4-(nitrogenous heteroaryl)-3,5-pyridine Dicarboxylates

Pier G. Baraldi, Roberta Budriesi, Barbara Cacciari, Alberto Chiarini, Laura Garuti, Giuseppe Giovanninetti, Alberto Leoni and Marinella Roberti

Dipartimento di Scienze Farmaceutiche, Università di Bologna, Via Belmeloro 6, 40126 Bologna, Italy


A new series of 4-(nitrogenous heteroaryl)-1,4-dihydropyridine antagonists II - XVI were synthesized and screened for inotropic, chronotropic and calcium antagonist properties, in order to evaluate the effect on pharmacological activity of replacement of the 4-aryl group of nifedipine-like drugs by heterocyclic moieties, such as quinoline, indole, carbazole and pyrazole. The most potent bradycardic compounds of the series (VIII - X, XII and XIII) elicited weak calcium antagonist activity and were stronger negative inotropic.