Preparation and pharmacological activities of spiro[3,4-dihydro-6/7-R-1,2,4-benzotriazine-3,4'-(1'-substituted)piperi dines].
A set of spiro[3,4-dihydro-1,2,4-benzotriazines-3,4'-piperidine] derivatives was prepared and subjected to a broad pharmacological screening. Many of these compounds are characterized by a 3-(4-fluorobenzoyl)propyl substituent on the piperidine nitrogen, thus resembling the p-fluorobutyrophenone antipsychotics. Modest dopamine antagonism was observed for the tested compounds, which however were mainly endowed with analgesic and antihypertensive activities. Antihypercholesterolemic activity was also seen in compound 5, which represents an interesting new lead, being completely structurally unrelated to the known agents in this field.
Novelli
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Istituto di Scienze Farmaceutiche, Università di Genova, Italy.
Sparatore
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D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D011918:Rats, Inbred SHR
D000700:Analgesics; D000924:Anticholesteremic Agents; D000959:Antihypertensive Agents; D018492:Dopamine Antagonists; D010880:Piperidines