16223-24-8Relevant academic research and scientific papers
A novel synthesis of N-(piperidin-4-yl)-1,3-dihydroindol-2-one via an intramolecular Pd-catalyzed amination
Van Den Hoogenband, Adri,Den Hartog, Jack A.J.,Lange, Jos H.M.,Terpstra, Jan Willem
, p. 8535 - 8537 (2004)
A novel efficient synthetic route to the pharmaceutical key intermediate N-(piperidin-4-yl)-1,3-dihydroindol-2-one is described. The key step involves a high-yielding intramolecular palladium-catalyzed amination reaction using Buchwald's X-Phos ligand und
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
Zaveri, Nurulain T.,Jiang, Faming,Olsen, Cris,Polgar, Willma E.,Toll, Lawrence
, p. 3308 - 3313 (2013/06/27)
The nociceptin receptor (NOP) and its endogenous agonist, nociceptin/orphanin FQ (N/OFQ), members of the opioid receptor and peptide families respectively, modulate the pharmacological effects of classical opioids, particularly opioid-induced reward and nociception. We hypothesized that compounds containing both NOP and opioid receptor activity in a single molecule may have useful pharmacological profiles as non-addicting analgesics or as drug abuse medications. We report here our forays into the structure-activity relationships for discovering 'bifunctional' NOP-mu opioid receptor (MOP) ligands, starting from our NOP-selective scaffolds. This initial SAR suggests pharmacophoric elements that may be modified to modulate/increase opioid affinity, while maintaining high affinity for the NOP receptor, to result in potent bifunctional small-molecule NOP/MOP ligands.
Piperidine amides as 11β-hydroxysteroid dehydrogenase type 1 inhibitors
Flyrén, Katarina,Bergquist, Lars O.,Castro, Victor M.,Fotsch, Christopher,Johansson, Lars,St. Jean Jr., David J.,Sutin, Lori,Williams, Meredith
, p. 3421 - 3425 (2008/02/08)
A series of piperidine amide inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) were identified via modifications of the HTS hit compound 1. The synthesis, in vitro biological evaluation, and structure-activity relationship of these co
AGONIST AND ANTAGONIST LIGANDS OF THE NOCICEPTIN RECEPTOR
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, (2008/06/13)
Novel piperidyl indolinone compounds are provided that are useful as agonist and antagonist ligands of the nociceptin receptor. The compounds are useful to treat a variety of disorders, and are particularly useful as analgesics.
