Artículos de revistas
Efecto de Piridazino (4-5-b)indoles en Trombano Sintetasa
Autor
Monge, Antonio
Aldana, Ignacio
Erro, A.
Parrado, P.
Font, M.
Rocha, E.
Prieto, I.
Fremont-Smith, M.
Fernández-Alvárez, E.
Institución
Resumen
Se han realizado los ensayos como inhibidores selectivos de Tromboexa no Sintetasa de siete comouestos de éstructura relativa a piridazino (45-b)indol. La inhibición en la segunda onda de agregación inducida en plaquetas humanas por
ADP, en la inducida por ácido araquidónico y por prostaglandina H<sub>2</sub> (PGH<sub>2</sub>), así
como en la producción de Tromboxano B<sub>2</sub> (TXB<sub>2</sub>), han permitido determinar que
dos de estos compuestos, 3,4-dihidro-4-oxo-5H-piridazino (4,5-b)indol (I) y 3,4-dihidro-4-oxo-5H-8-benciloxi-piridazino (4, 5-b)indol (VII), son nuevos inhibidores selectivos de este sistema enzimático. Assays were performed which identified seven compounds with the general structure indol-piridazine (4,5-b) as selective inhibitors of Thromboxane Synthetase. Compounds whose activities includes inhibition of human platelet aggregation induced by Arachidonic acid (AA) and Prostaglandin H<sub>2</sub> (PGH<sub>2</sub>), and inhibition of the second wave of platelet aggregation induced by ADP, were subjected to radioimmunoassay studies to measue TXB<sub>2</sub> and PGE<sub>2</sub> levels in the samples using AA as the aggregating agent. This work has determined that two of the compounds, 3,4-dihydro-4-oxo-5H-pyridazino-(4,5-b)indole(I) and 3,4-dihydro-4-oxo-5H 8-benzyloxypyridazino (4,5-b)indole (VII), are new selective inhibitors of this enzymatic system