Synthesis and pharmacological characterization of some benzazepinone derivatives.
A series of some benzazepinone derivatives were prepared. The compounds were evaluated for inotropic, chronotropic and calcium antagonist properties. For the compounds bearing well-known alpha-blocking fragments, the antagonist potency at postsynaptic alpha-adrenoceptors was assessed. The new compounds were less effective as bradycardic agents and calcium antagonists but show remarkable negative inotropic activity.
Budriesi
R
R
Department of Pharmaceutical Sciences, University of Bologna, Italy.
Rampa
A
A
Bisi
A
A
Fabbri
G
G
Chiarini
A
A
Valenti
P
P
D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects; D001552:Benzazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D006325:Heart Atria / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D013329:Structure-Activity Relationship
D000317:Adrenergic alpha-Antagonists; D001552:Benzazepines; D002121:Calcium Channel Blockers; D002316:Cardiotonic Agents