Cardiovascular hybrid drugs: New benzazepinone derivatives as bradycardic agents endowed with selective beta(1)-non-competitive antagonism
Articolo
Data di Pubblicazione:
2003
Citazione:
Cardiovascular hybrid drugs: New benzazepinone derivatives as bradycardic agents endowed with selective beta(1)-non-competitive antagonism / A. Bisi, A. Rampa, R. Budriesi, S. Gobbi, F. Belluti, P. Ioan, E. Valoti, A. Chiarini, P. Valenti. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 11:7(2003), pp. 1353-1361.
Abstract:
The synthesis and pharmacological profile of some hybrid compounds
bearing both the benzazepinone moiety present in Zatebradine and typical P-blocker aryloxypropanolamine groups are described. The new compounds
proved to be endowed with negative chronotropic and inotropic activity
and are weak vasorelaxant agents. The cardiodepressant action is
probably due to selective beta(1)-noncompetitive reversible antagonism. Both enantiomers of the most active compound 5c were synthesized and they showed a different cardiovascular profile, that is
(+)-(R)-enantiomer displays affinity for cardiac beta(1)-adrenoceptors,
while (-)-(S)-enantiomer shows specificity for vessel smooth muscle.
Tipologia IRIS:
01 - Articolo su periodico
Elenco autori:
A. Bisi, A. Rampa, R. Budriesi, S. Gobbi, F. Belluti, P. Ioan, E. Valoti, A. Chiarini, P. Valenti
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