Synthesis and .alpha.-D-glucosidase inhibitory activity of N-substituted valiolamine derivatives as potential oral antidiabetic agents
作者:Satoshi Horii、Hiroshi Fukase、Takao Matsuo、Yukihiko Kameda、Naoki Asano、Katsuhiko Matsui
DOI:10.1021/jm00156a023
日期:1986.6
in this study have been found to be more potent than the corresponding N-substituted valienamine derivatives as well as the parent valiolamine. It is noteworthy that even simple N-substituted valiolamine derivatives such as N-[2-hydroxy-1-(hydroxymethyl)ethyl]-, N-[(1R,2R)-2-hydroxycyclohexyl]-, and N-[(R)-(-)-beta-hydroxyphenethyl]valiolamine (6, 8a, and 9a) have the stronger alpha-D-glucosidase inhibitory
合成了各种N-取代的缬氨酰胺衍生物,包括化合物23a,24a和34a,其结构类似于天然存在的寡糖α-D-葡萄糖苷酶抑制剂的关键假二糖(25a和26a)。对猪蔗糖酶和麦芽糖酶的抑制活性。已经发现,在这项研究中评估的N-取代缬胺胺衍生物比相应的N-取代缬胺胺衍生物和母体缬胺胺更有效。值得注意的是,即使是简单的N-取代的缬胺胺衍生物,例如N- [2-羟基-1-(羟甲基)乙基]-,N-[((1R,2R)-2-羟基环己基]-和N-[(R )-(-)-β-羟基苯乙基]缬胺(6,8a,