Novel imidazole derivatives with subtype-selective antimuscarinic activity (1).
A series of N-substituted 4-amino-2,2-diphenylbutyramide derivatives was prepared as part of a search for subtype-selective antimuscarinic agents. The representative compound KRP-197, bearing a 2-methylimidazole ring as a surrogate of aliphatic amine, was found to be a highly potent and both M1- and M3-selective antimuscarinic agent.
Miyachi
H
H
Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd., Tochigi, Japan.
Kiyota
H
H
Segawa
M
M
D000818:Animals; D006168:Guinea Pigs; D006325:Heart Atria / Q000187:drug effects; D007082:Ileum / Q000187:drug effects; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D015394:Molecular Structure; D018727:Muscarinic Antagonists / Q000737:chemistry / Q000494:pharmacology*; D011817:Rabbits; D014649:Vas Deferens / Q000187:drug effects
D007093:Imidazoles; D018727:Muscarinic Antagonists