Synthesis and preliminary pharmacological evaluation of 3-[2-(1-aryl-piperazin-4-yl)ethyl]-3,4-dihydro-3-methyl-6-R-1,2, 4-benzotriazines.
A set of 3-[2-(1-aryl-piperazin-4-yl)ethyl]-3,4-dihydro-3-methyl-1,2, 4-benzotriazines, bearing different substituents on the aromatic nuclei, was prepared and found to be endowed with good antihypertensive activity. The simplest compound 1, subjected to a broad pharmacological screening, exhibited also analgesic and antiallergic activities and hints of hypocholesterolemic action. Moreover this compound inhibited (in vitro tests) the guinea pig ileum contractions induced by several agents, the rat vas deferens contractions induced by phenylphrine (alpha 1 antagonism), the platelet aggregation induced by arachidonate and the tracheal tone.
Novelli
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Istituto di Scienze Farmaceutiche, Università di Genova, Italy.
Sparatore
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D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D008297:Male; D051379:Mice; D051381:Rats; D011918:Rats, Inbred SHR; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000494:pharmacology
D000959:Antihypertensive Agents; D014227:Triazines