一些取代的2-芳基噻唑并[3,2-a]吡啶鎓盐的合成及降血糖活性

Synthesis and hypoglycemic activity of some substituted 2-arylthiazolo[3,2-a]pyridinium salts.

作者信息

Blank B, DiTullio N W, Krog A J, Saunders H L

出版信息

J Med Chem. 1978 May;21(5):489-92. doi: 10.1021/jm00203a019.

Abstract

A series of substituted 2-arylthiazolo[3,2-a]pyridinium salts (1a-q) was prepared by known methods and tested for hypoglycemic activity in 48-h fasted rats. Two compounds, 2-phenylthiazolo- and 8-methyl-2-phenythiazolo[3,2-a]pyridinium perchlorate (1a and 1q), showed consistent hypoglycemic activity in this screen, demonstrating that a high degree of structural specificity was required for hypoglycemic activity. At higher doses the hypoglycemic activity of 1a and 1q was associated with elevated levels of hepatic triglycerides.

摘要

通过已知方法制备了一系列取代的2-芳基噻唑并[3,2-a]吡啶鎓盐（1a-q），并在禁食48小时的大鼠中测试其降血糖活性。两种化合物，2-苯基噻唑并-和8-甲基-2-苯基噻唑并[3,2-a]吡啶鎓高氯酸盐（1a和1q），在此筛选中显示出一致的降血糖活性，表明降血糖活性需要高度的结构特异性。在较高剂量下，1a和1q的降血糖活性与肝脏甘油三酯水平升高有关。