4-Substituted anilides as selective melatonin MT2 receptor agonists

A series of 4-substituted anilides with human melatonergic affinity is reported. Butyramides 26, 39, 42, 52, 57, and 58 all demonstrated subnanomolar MT(2) binding affinity and MT(2) selectivity of at least 70-fold over the MT(1) receptor. Compound 26 demonstrated full agonism at the MT(2) receptor.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-02, Vol.14 (4), p.1023-1026
Hauptverfasser:	EPPERSON, James R, DESKUS, Jeffrey A, GENTILE, Anthony J, IBEN, Lawrence G, RYAN, Elaine, SARBIN, Nathan S
Format:	Artikel
Sprache:	eng
Schlagworte:	Anilides - chemical synthesis Anilides - chemistry Binding, Competitive Biological and medical sciences Hormones. Endocrine system Humans Medical sciences Melatonin - metabolism Molecular Structure Pharmacology. Drug treatments Receptor, Melatonin, MT2 - agonists Receptor, Melatonin, MT2 - chemistry Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	A series of 4-substituted anilides with human melatonergic affinity is reported. Butyramides 26, 39, 42, 52, 57, and 58 all demonstrated subnanomolar MT(2) binding affinity and MT(2) selectivity of at least 70-fold over the MT(1) receptor. Compound 26 demonstrated full agonism at the MT(2) receptor.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2003.11.030