Discovery of 1-Butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): A Novel Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor was written by Cid, Jose Maria;Tresadern, Gary;Duvey, Guillaume;Lutjens, Robert;Finn, Terry;Rocher, Jean-Philippe;Poli, Sonia;Vega, Juan Antonio;de Lucas, Ana Isabel;Matesanz, Encarnacion;Linares, Maria Lourdes;Andres, Jose Ignacio;Alcazar, Jesus;Alonso, Jose Manuel;Macdonald, Gregor J.;Oehlrich, Daniel;Lavreysen, Hilde;Ahnaou, Abdelah;Drinkenburg, Wilhelmus;Mackie, Claire;Pype, Stefan;Gallacher, David;Trabanco, Andres A.. And the article was included in Journal of Medicinal Chemistry in 2014.Recommanded Product: 4-(2-Methoxyphenyl)piperidine This article mentions the following:
The authors previously reported the discovery of 4-aryl-substituted pyridones with mGlu2 PAM activity starting from the HTS hit I. In this article, the authors describe a different exploration I from that led to the discovery of a novel subseries of phenylpiperidine-substituted pyridones. The optimization strategy involved the introduction of different spacers between the pyridone core and the Ph ring of I. The fine tuning of metabolism and hERG followed by differentiation of advanced leads that were identified on the basis of PK profiles and in vivo potency converged on lead compound II (JNJ-40411813). Full in vitro and in vivo profiles indicate that II displayed an optimal interplay between potency, selectivity, favorable ADMET/PK and cardiovascular safety profile, and central EEG activity. Compound II has been investigated in the clinic for schizophrenia and anxious depression disorders. In the experiment, the researchers used many compounds, for example, 4-(2-Methoxyphenyl)piperidine (cas: 58333-75-8Recommanded Product: 4-(2-Methoxyphenyl)piperidine).
4-(2-Methoxyphenyl)piperidine (cas: 58333-75-8) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Recommanded Product: 4-(2-Methoxyphenyl)piperidine
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem