Pyrimidine derivatives. VI. Synthesis of 2-(1-piperazinyl)-5,6-polymethylenepyrimidine derivatives and determination of their hypoglycemic activity.
作者:TETSUO SEKIYA、HIDETOSHI HIRANUMA、TOSHIJI KANAYAMA、SHUNSUKE HATA、SHUNICHI YAMADA
DOI:10.1248/cpb.31.2254
日期:——
As part of our studies on pyrimidine derivatives, 27 4-alkyl-2-(1-piperazinyl)-5, 6-polymethylenepyrimidines and structurally related derivatives were synthesized, and their hypoglycemic activities were examined in mice treated with 2-deoxy-D-glucose. Most of the derivatives showed higher activity at a dose of 30 mg/kg p.o. than tolbutamide at a dose of 100 mg/kg p.o. The structure-activity relationships are discussed.
作为我们对嘧啶衍生物研究的一部分,我们合成了27种4-烷基-2-(1-哌嗪基)-5, 6-多甲基化嘧啶及其结构相关衍生物,并检测了其在接受2-脱氧-D-葡萄糖处理的小鼠中的降血糖活性。大多数衍生物在30 mg/kg口服剂量下显示出比100 mg/kg口服剂量的噻唑安更高的活性。讨论了结构-活性关系。