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

Author:

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

Abstract

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.

Publisher

Institute of Organic Chemistry & Biochemistry

Subject

General Chemistry

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