Synthesis of N-(carbonylamino)-1,2,3,6-tetrahydropyridines with analgesic, antiinflammatory, and hyperglycemic activity
作者:Jupita M. Yeung、Linda A. Corleto、Edward E. Knaus
DOI:10.1021/jm00344a020
日期:1982.2
the effects that changes in functionality at the carbonyl group have on analgesic, antiinflammatory, and hyperglycemic activities. One of the most active analgesic compounds was N-[(ethoxycarbonyl)amino]-1,2,3,6-tetrahydropyridine (5o), which was comparable to that of morphine. Pretreatment with naloxone did not alter the activity of 5o or 5q. N-[(2-Furanylcarbonyl)amino]-1,2,3,6-tetrahydropyridine (5q)
合成了一组N-(羰基氨基)-1,2,3,6-四氢吡啶,以研究羰基官能团的变化对镇痛,抗炎和高血糖活性的影响。活性最高的镇痛化合物之一是N-[(乙氧羰基)氨基] -1,2,3,6-四氢吡啶(5o),与吗啡相当。纳洛酮预处理不会改变5o或5q的活性。N-[(2-呋喃基羰基)氨基] -1,2,3,6-四氢吡啶(5q)是最有效的降血糖药,在100 mg / kg po剂量后第2和第4小时血糖升高181%。