96254-71-6Relevant academic research and scientific papers
Cardiovascular hybrid drugs: New benzazepinone derivatives as bradycardic agents endowed with selective β1-Non-competitive antagonism
Bisi, Alessandra,Rampa, Angela,Budriesi, Roberta,Gobbi, Silvia,Belluti, Federica,Ioan, Pierfranco,Valoti, Ermanno,Chiarini, Alberto,Valenti, Piero
, p. 1353 - 1361 (2003)
The synthesis and pharmacological profile of some hybrid compounds bearing both the benzazepinone moiety present in Zatebradine and typical β-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 β1-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 β1-adrenoceptors, while (-)-(S)-enantiomer shows specificity for vessel smooth muscle.
Synthesis and pharmacological characterization of some benzazepinone derivatives
Budriesi,Rampa,Bisi,Fabbri,Chiarini,Valenti
, p. 234 - 239 (2007/10/02)
A series of some benzazepinone derivatives were prepared. The compounds were evaluated for inotropic, chronotropic and calcium antagonist properties. For the compounds bearing wel-known α-blocking fragments, the antagonist potency at postsynaptic α-adrenoceptors was assessed. The new compounds were less effective as bradycardic agents and calcium antagonists but show remarkable negative inotropic activity.
