Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.
A series of alpha1a receptor antagonists derived from a 4-aryl-3,4-dihydropyridine-2-one heterocycle is disclosed. Potency in the low nanomolar to picomolar range along with high selectivity was obtained. In vivo efficacy in a prostate contraction model in rats was observed with a few derivatives.
Department of Medicinal Chemistry, Merck & Co., West Point, PA 19486, USA. philippe_nantermet@merck.com
P G
PG
Nantermet
J C
JC
Barrow
H G
HG
Selnick
C F
CF
Homnick
R M
RM
Freidinger
R S
RS
Chang
S S
SS
O'Malley
D R
DR
Reiss
T P
TP
Broten
R W
RW
Ransom
D J
DJ
Pettibone
T
T
Olah
C
C
Forray
D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D004095:Dihydropyridines / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats
D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists; D004095:Dihydropyridines