Synthesis and cardiodepressant activity of dialkyl 1,4-dihydro-2,6-dimethyl-4-(pentatomic-heteroaryl)-3,5-pyridine-dicarbo xylates. 2.
A new series of 1,4-dihydropyridine bearing substituted pyrazole and imidazole at C-4 position was synthesized and characterized as inotropic, chronotropic and calcium antagonist agents, in order to evaluate the effect on pharmacological activity of replacement of the 4-aryl group of nifedipine-like drugs by pyrazole and imidazole moieties. All compounds were tested on myocardial muscle and vascular smooth muscle of guinea-pigs. The new compounds showed both significant selective negative inotropic activity and fairly good negative chronotropic effects. All compounds elicited weak calcium antagonist activity, except compound 9 which is a selective bradycardic agent.
Baraldi
P G
PG
Dipartimento di Scienze Farmaceutiche, Università di Bologna, Italy.
Garuti
L
L
Leoni
A
A
Cacciari
B
B
Budriesi
R
R
Chiarini
A
A
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002121:Calcium Channel Blockers / Q000494:pharmacology; D004095:Dihydropyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D009993:Osmium Tetroxide / Q000737:chemistry; D013329:Structure-Activity Relationship
D000889:Anti-Arrhythmia Agents; D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D009993:Osmium Tetroxide