Sanna P, Loriga M, Cignarella G, Ferni G
Farmaco Sci. 1985 Jul;40(7):477-85. doi: 10.1002/chin.198546198.
The synthesis of a new series of 1-alkoxybenzyl-4-(2-pyrimidyl)piperazines 2-methyl or 2,6-dimethyl substituted, related to piribedil, is described. Besides compounds (IV)-(IX a, b), the isomer (XI) of (V) was also prepared. Central dopaminergic and alpha-blocking activities both in vitro and in vivo were determined for all compounds. Derivatives (IV), (VII), (XI) were also studied for peripheral vasodilator and sympatholytic activities.
描述了与匹立地尔相关的一系列新的1-烷氧基苄基-4-(2-嘧啶基)哌嗪的合成，这些哌嗪为2-甲基或2,6-二甲基取代。除了化合物(IV)-(IX a,b)外，还制备了(V)的异构体(XI)。测定了所有化合物的体外和体内中枢多巴胺能活性及α-阻断活性。还研究了衍生物(IV)、(VII)、(XI)的外周血管舒张活性和抗交感神经活性。
