A novel series of N-(1-aminoalkylidene)carboximidamides as potential hypoglycemia agents
作者:Henry J. Breslin、Michael J. Kukla、Robert W. Tuman、Mary C. Rebarchak、Charles R. Bowden
DOI:10.1021/jm00063a009
日期:1993.5
Nitrogen heterocyclic carboximidamides, such as linogliride, 1a, have been shown to possess significant hypoglycemic activity and have shown clinical efficacy as potential antidiabetic agents. We evaluated the biological significance of the heterocyclic ring A of general structure 1, which has always been maintained in this class of compounds, by preparing acyclic compounds of general structure 2.
氮杂环羧酰亚胺类化合物(如linogliride,1a)已显示出显着的降血糖活性,并已显示出作为潜在抗糖尿病药的临床疗效。我们通过制备通用结构2的无环化合物,评估了通用结构1的杂环A的生物学意义。该结构在此类化合物中一直保持着。初步的体内生物学测试,即大鼠的葡萄糖耐量测试,指出,制备的许多特定的无环羧酰亚胺化合物6a-kk具有显着的降血糖活性,通常与我们的模型化合物1a所示的活性相当,在某些情况下更好。这些结果表明1的杂环A对于这类化合物的降血糖活性不是必需的。