Cardiotonic agents. 1-Methyl-7-(4-pyridyl)-5,6,7,8-tetrahydro-3(2H)-isoquinolinones and related compounds. Synthesis and activity
| Autor: | Kengo Otsuka, Masahiko Maruyama, Seitaro Kajiya, Toshihiko Ito, Kunio Sannohe, Joji Kamiya, Tatsuo Kaiho, Tsuneji Suzuki |
|---|---|
| Rok vydání: | 1989 |
| Předmět: |
Male
Inotrope Cardiotonic Agents Pyridines Medicinal chemistry Contractility Structure-Activity Relationship Dogs Drug Discovery Heart rate medicine Animals Structure–activity relationship heterocyclic compounds Chemistry organic chemicals Isoquinolines medicine.disease Myocardial Contraction Blood pressure Heart failure Molecular Medicine Milrinone Female medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry. 32:351-357 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00122a012 |
| Popis: | A series of 1-methyl-7-(4-pyridyl)-5,6,7,8-tetrahydro-3(2H)-isoquinolinones and related compounds were synthesized and evaluated for positive inotropic activity. Most members of this series exerted a dose-dependent increase in myocardial contractility in the dog acute heart failure model, whereas they caused only slight changes in heart rate and blood pressure. Several derivatives, especially those with cyano, acetyl, and ethyl substituents at the 4-position, were more potent than milrinone, which was used as a reference. 4-Acetyl-1-methyl-7-(4-pyridyl)-5,6,7,8-tetrahydro-3(2H)-isoquinolinone (MS-857) is one of the most potent positive inotropic agents in this series. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|