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New aminocarboxamides with class III anti-arrhythmic activity
H Poppe1, R Schindler, W Sauer
1Department of Chemistry, Corporate R & D, Arzneimittelwerk Dresden GmbH, Radebeul, Germany.
Archiv Der Pharmazie
|August 18, 1999
Summary
New aminocarboxamides demonstrate Class III anti-arrhythmic activity by prolonging the effective refractory period. Certain compounds show promise for treating cardiac arrhythmias, particularly after myocardial infarction and in atrial fibrillation.
Area of Science:
- Pharmacology
- Cardiovascular Medicine
- Medicinal Chemistry
Background:
- Aminocarboxamides represent a novel class of compounds investigated for anti-arrhythmic properties.
- Class III anti-arrhythmics function by prolonging the cardiac effective refractory period (ERP).
Purpose of the Study:
- To synthesize and characterize novel aminocarboxamides with potential Class III anti-arrhythmic activity.
- To evaluate the efficacy of these compounds in prolonging action potential duration (APD) and ERP in vitro and in vivo.
Main Methods:
- Chemical synthesis of aminocarboxamide derivatives.
- In vitro electrophysiological studies on guinea pig papillary muscles to assess APD and ERP.
- In vivo electrophysiological characterization in animal models (dogs, rabbits) to determine anti-arrhythmic and pro-arrhythmic effects.
Main Results:
- Several aminocarboxamides demonstrated Class III activity, prolonging ERP, with some showing greater effects at faster stimulation rates.
- AWD 160-275 (13) effectively prevented arrhythmias in dogs, suggesting utility post-myocardial infarction.
- AWD 23-111 (14) exhibited a low pro-arrhythmic effect compared to existing Class III agents.
Conclusions:
- Aminocarboxamides are a promising new class of Class III anti-arrhythmic agents.
- Specific derivatives, like AWD 160-275, show potential for treating serious cardiac arrhythmias.
- These findings warrant further investigation for therapeutic applications in cardiovascular disease.