Opioid Receptor Modulators with a Cinnamyl Group

To obtain selective and potent opioid receptor ligands, we synthesized dehydro derivatives of alvimopan and found compound (28f), a selective but modest affinity MOR antagonist weaker than alvimopan (1). We replaced the arylpiperidine unit by an arylpiperazine to obtain the 1-(α-carboxycinnamyl)-4-a...

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Veröffentlicht in:	Journal of medicinal chemistry 2017-08, Vol.60 (15), p.6733-6750
Hauptverfasser:	Ravilla, Lokesh, Venkata subba Naidu, N, Dogra, Shalini, Umrao, Deepmala, Yadav, Prem N, Biswas, Ansuman, Michael, Daliah, Sekar, Kanagaraj, Nagarajan, Kuppuswamy
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Blood-Brain Barrier - metabolism Cinnamates - chemical synthesis Cinnamates - pharmacology HEK293 Cells Humans Ligands Male Mice, Inbred C57BL Molecular Docking Simulation Naloxone - pharmacology Narcotic Antagonists - chemical synthesis Narcotic Antagonists - pharmacology Piperazines - chemical synthesis Piperazines - pharmacology Piperidines - chemical synthesis Piperidines - pharmacology Receptors, Opioid, kappa - agonists Receptors, Opioid, mu - antagonists & inhibitors
Online-Zugang:	Volltext
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