Synthesis, in vitro [3H]prazosin displacement, and in vivo activity of 3-aryl-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridines, a new class of antihypertensive agents
作者:Giorgio Winters、Alberto Sala、Domenico Barone、Emiliana Baldoli
DOI:10.1021/jm00145a015
日期:1985.7
A series of new 3-aryl-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridines was synthesized and screened for in vitro [3H]prazosin displacement activity. The results correlated well with their antihypertensive activity in spontaneous hypertensive rats. 1-Benzyl-3-(4-fluorophenyl)-4,5,6,7-tetrahydropyrazolo[4,3-c]pyrid ine (50, L 16052) was selected for further pharmacological evaluations of its potency when administered orally to conscious renal hypertensive dogs.