4-Aroyl-1,3-dihydro-2H-imidazol-2-ones, a new class of cardiotonic agents
| Autor: | J M Grisar, R A Schnettler, Richard C. Dage |
|---|---|
| Rok vydání: | 1982 |
| Předmět: |
Inotrope
Male Pentobarbital Cardiac output Cardiotonic Agents Chemical Phenomena Blood Pressure Propranolol Pharmacology Dogs Heart Rate Drug Discovery medicine Animals Cardiac Output Chemistry Hemodynamics Imidazoles Biological activity medicine.disease Myocardial Contraction Blood pressure Heart failure Molecular Medicine Female medicine.drug |
| Zdroj: | Journal of medicinal chemistry. 25(12) |
| ISSN: | 0022-2623 |
| Popis: | A series of 4-aroyl-1,3-dihydro-2H-imidazol-2-ones was synthesized and evaluated for pharmacological activity in the anesthetized dog. Most members of this series produced dose-related increases in cardiac contractile force as well as relatively minor increases in heart rate and decreases in systemic arterial blood pressure that were not blocked by propranolol. In general, 4-methoxy or 4-methylthiobenzoyl substitution afforded compounds of greatest inotropic potency. 1,3-Dihydro-4-(4-methoxybenzoyl)-5-methyl-2H-imidazol-one (6) was shown to produce a dose-related positive inotropic effect and reverse the depressant effect of pentobarbital on cardiac pump function in the dog heart-lung preparation. The cardiotonic activity of this series may have important utility in the treatment of congestive heart failure. 1,3-Dihydro-4-[4-(methylthio)benzoyl]-5-methyl-2H-imidazol-2-one (17) was chosen for human studies and is currently undergoing clinical trials. |
| Databáze: | OpenAIRE |
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