Design and synthesis of 3-arylpyrrolidine-2-carboxamide derivatives as melanocortin-4 receptor ligands

Based on 3-phenylpropionamides, a series of 3-arylpyrrolidine-2-carboxamide derivatives was designed and synthesized to study the effect of cyclizations as melanocortin-4 receptor ligands. It was found that the 2 R,3 R-pyrrolidine isomer possessed the most potent affinity among the four stereoisomer...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-03, Vol.18 (6), p.1931-1938
Hauptverfasser:	Tran, Joe A., Tucci, Fabio C., Arellano, Melissa, Jiang, Wanlong, Chen, Caroline W., Marinkovic, Dragan, Fleck, Beth A., Wen, Jenny, Foster, Alan C., Chen, Chen
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Biological and medical sciences Biological Availability Brain - drug effects Cyclization Drug Design Medical sciences Melanocortin-4 receptor Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Pyrrolidine Pyrrolidines - chemical synthesis Pyrrolidines - chemistry Pyrrolidines - pharmacokinetics Pyrrolidines - pharmacology Rats Receptor, Melanocortin, Type 4 - agonists Receptor, Melanocortin, Type 4 - metabolism Stereoisomer Stereoisomerism Structure-Activity Relationship Synthesis
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Beschreibung
Zusammenfassung:	Based on 3-phenylpropionamides, a series of 3-arylpyrrolidine-2-carboxamide derivatives was designed and synthesized to study the effect of cyclizations as melanocortin-4 receptor ligands. It was found that the 2 R,3 R-pyrrolidine isomer possessed the most potent affinity among the four stereoisomers.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2008.01.125