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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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 14; no. 4; pp. 1023 - 1026
Main Authors EPPERSON, James R, DESKUS, Jeffrey A, GENTILE, Anthony J, IBEN, Lawrence G, RYAN, Elaine, SARBIN, Nathan S
Format Journal Article
LanguageEnglish
Published Oxford Elsevier 23.02.2004
Subjects
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
Human
Agonist
Structure activity relation
Carboxamide
Selectivity
MT2 melatonin receptor
Chemical synthesis
In vitro
Anilide
Hormonal receptor
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Summary: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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.11.030