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 was written by 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.. And the article was included in Journal of Medicinal Chemistry in 2009.Category: piperazines This article mentions the following:
N-(3-Fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine 12 (GSK962040) is a novel small mol. 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. In the experiment, the researchers used many compounds, for example, (R)-1-Cbz-2-methylpiperazine (cas: 923565-99-5Category: piperazines).
(R)-1-Cbz-2-methylpiperazine (cas: 923565-99-5) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Category: piperazines
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics