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.
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.
Winters
G
G
Sala
A
A
Barone
D
D
Baldoli
E
E
D000818:Animals; D001921:Brain / Q000378:metabolism; D002415:Cats; D055598:Chemical Phenomena; D002621:Chemistry; D004285:Dogs; D006973:Hypertension / Q000188:drug therapy*; D006978:Hypertension, Renovascular / Q000188:drug therapy; D008297:Male; D051379:Mice; D011224:Prazosin / Q000378:metabolism*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000378:metabolism / Q000627:therapeutic use*; D011725:Pyridines / Q000138:chemical synthesis / Q000378:metabolism / Q000627:therapeutic use*; D011799:Quinazolines / Q000378:metabolism*; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism; D013329:Structure-Activity Relationship; D013574:Synaptosomes / Q000378:metabolism
D011720:Pyrazoles; D011725:Pyridines; D011799:Quinazolines; D011942:Receptors, Adrenergic, alpha; D011224:Prazosin