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Pinacidil是氰胍类钾通道启开剂的代表,1987年在丹麦首次上市,最近在美国得到批准用于治疗高血压。Pinacidil是一个较好的新型降压药,但是它的组织选择性较差,可引起一些副作用。本文根据Pinacidil类化合物的定量构效关系(QSAR),设计并合成了8个氰胍和4个硫脲类化合物,分离鉴定了三个亚胺类副产物,它们是2-(2’-甲基哌啶基)-4-(甲硫基-3’-吡啶氨基)双亚胺(BP01),2-(3’-甲基哌啶基)-4-(甲硫基-3’-吡啶氨基)双亚
Pinacidil is the representative of the cyanidinium potassium channel opener, first introduced in Denmark in 1987 and recently approved in the United States for the treatment of hypertension. Pinacidil is a better new antihypertensive drug, but its poor tissue selectivity can cause some side effects. According to the quantitative structure-activity relationship (QSAR) of Pinacidil compounds, we designed and synthesized 8 metaguanidines and 4 thiourea compounds. Three imine byproducts were isolated and identified as 2- (2’-A (Methylthio-3’-pyridylamino) bisimine (BP01), 2- (3’-methylpiperidinyl) -4- (methylthio-3’-pyridine Amino) subunit