Novelli F, Sparatore F
Istituto di Scienze Farmaceutiche, Università di Genova, Italy.
Farmaco. 1996 Aug-Sep;51(8-9):541-50.
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.
制备了一组螺[3,4-二氢-1,2,4-苯并三嗪-3,4'-哌啶]衍生物，并进行了广泛的药理筛选。这些化合物中的许多在哌啶氮上具有3-(4-氟苯甲酰基)丙基取代基，因此类似于对氟丁酰苯类抗精神病药。测试的化合物表现出适度的多巴胺拮抗作用，然而它们主要具有镇痛和降压活性。化合物5还表现出抗高胆固醇血症活性，它代表了一个有趣的新先导物，在结构上与该领域已知药物完全无关。
