Structure–activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor

[Display omitted] A series of cyclohexylpiperazines was synthesized as potent and selective antagonists of the human MC4 receptor. Compound 14t displayed binding affinity ( K i) of 4.2 and 1100 nM at MC4R and MC3R, respectively.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-07, Vol.15 (14), p.3434-3438
Hauptverfasser:	Tran, Joseph A., Pontillo, Joseph, Arellano, Melissa, Fleck, Beth A., Tucci, Fabio C., Marinkovic, Dragan, Chen, Caroline W., Saunders, John, Foster, Alan C., Chen, Chen
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemistry Antagonist Binding, Competitive Biological and medical sciences Cyclohexylpiperazine Humans Medical sciences Melanocortin-4 receptor Molecular Conformation Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacology Receptor, Melanocortin, Type 3 - antagonists & inhibitors Receptor, Melanocortin, Type 4 - antagonists & inhibitors Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	[Display omitted] A series of cyclohexylpiperazines was synthesized as potent and selective antagonists of the human MC4 receptor. Compound 14t displayed binding affinity ( K i) of 4.2 and 1100 nM at MC4R and MC3R, respectively.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.05.017