Journal of medicinal chemistry, 2003-03, Vol.46 (7), p.1127-1129
2003
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Details
- Autor(en) / Beteiligte
- Titel
- Design and Synthesis of Naphthalenic Dimers as Selective MT1 Melatoninergic Ligands
- Ist Teil von
- Journal of medicinal chemistry, 2003-03, Vol.46 (7), p.1127-1129
- Ort / Verlag
- United States: American Chemical Society
- Erscheinungsjahr
- 2003
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- We report the synthesis and binding properties at MT1 and MT2 receptors of the first example of agomelatine (N-[2-(7-methoxynaphth-1-yl)ethyl]acetamide) dimers in which two agomelatine moieties are linked together through their methoxy substituent by a polymethylene side chain according to the “bivalent ligand” approach. Some of these compounds behave as MT1-selective ligands. The most selective one (5) behaves as an antagonist.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0022-2623eISSN: 1520-4804DOI: 10.1021/jm0255872Titel-ID: cdi_proquest_miscellaneous_73121675
- Format
- –
- Schlagworte
- Acetamides - chemistry, Acetamides - pharmacology, Animals, Cell Line, Cricetinae, Dimerization, Drug Design, Humans, Ligands, Melatonin - metabolism, Naphthalenes - chemical synthesis, Naphthalenes - chemistry, Naphthalenes - pharmacology, Radioligand Assay, Receptors, Cell Surface - agonists, Receptors, Cell Surface - antagonists & inhibitors, Receptors, Cell Surface - drug effects, Receptors, Cytoplasmic and Nuclear - agonists, Receptors, Cytoplasmic and Nuclear - antagonists & inhibitors, Receptors, Cytoplasmic and Nuclear - drug effects, Receptors, Melatonin, Structure-Activity Relationship