Journal of medicinal chemistry · 2009
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.
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Westaway Susan M, Brown Samantha L, Fell Stephen C M, Johnson Christopher N, MacPherson David T, Mitchell Darren J, Myatt James W, Stanway Steven J, Seal Jon T, Stemp Geoffrey, Thompson Mervyn, Lawless Kirk, McKay Fiona, Muir Alison I, Barford Jonathan M, Cluff Chermaine, Mahmood Sadhia R, Matthews Kim L, Mohamed Shiyam, Smith Beverley, Stevens Alexander J, Bolton Victoria J, Jarvie Emma M, Sanger Gareth J
Аннотация
N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine 12 (GSK962040) is a novel small molecule motilin receptor agonist. It possesses excellent activity at the recombinant human motilin receptor and also at the native rabbit motilin receptor where its agonist activity results in potentiation of the amplitude of neuronal-mediated contractions of isolated gastric antrum tissue. Compound 12 also possesses highly promising pharmacokinetic profiles in both rat and dog, and these results, in combination with further profiling in human native tissue and an in vivo model of gastrointestinal transit in the rabbit, have led to its selection as a candidate for further development.