Pyrazole analogues of prazosin.
A series of analogues of prazosin, in which 1-methyl or 1-phenylpyrazole moieties were substituted for the furan ring, were synthesized and studied for their alpha 1-adrenoceptor antagonist activity. The role of the five member heterocyclic substructures in determining the affinity for the alpha 1-receptor is briefly discussed.
Ermondi
G
G
Dipartimento di Scienza e Tecnologia del Farmaco, Università di Torino, Turin, Italy.
Boschi
D
D
Di Stilo
A
A
Tironi
C
C
Gasco
A
A
D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D008958:Models, Molecular; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D011224:Prazosin / Q000031:analogs & derivatives*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
D000317:Adrenergic alpha-Antagonists; D011720:Pyrazoles; D011224:Prazosin