Journal ArticleDOI
5-substituted 3,4-dihydro-3-amino-2H-1-benzopyran derivatives: synthesis and interaction with serotoninergic receptors.
R. Rezaie,Benoît Joseph,J. B. Bremner,P Delagrange,C Kopp,René Misslin,B. Pfeiffer,Pierre Renard,G. Guillaumet +8 more
TLDR
A new series of 3,4‐dihydro‐3‐amino‐2H‐1‐benzopyran derivatives bearing various substituents on the 5‐position was successfully prepared via palladium‐mediated cross‐coupling reactions and some of the new compounds showed high affinity for 5‐HT1A and5‐HT7 receptors.Abstract:
A new series of 3,4-dihydro-3-amino-2H-1-benzopyran derivatives (1 and 2) bearing various substituents on the 5-position was successfully prepared via palladium-mediated cross-coupling reactions. Some of the new compounds showed high affinity for 5-HT1A and 5-HT7 receptors. The best affinity for the 5-HT1A and 5-HT7 receptors was obtained for 2b (Ki = 0.3 nM for 5-HT1A and 3.1 nM for 5-HT7). The anxiolytic activity of compound 2b was evaluated.read more
Citations
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Journal ArticleDOI
Synthesis of 3-Aminochroman Derivatives by Radical Cyclization
TL;DR: Enantiomeric purities of the final aminochroman derivatives were determined by capillary electrophoresis using beta-cyclodextrins as a chiral selector.
Journal ArticleDOI
New 1-arylindoles based serotonin 5-HT7 antagonists. Synthesis and binding evaluation studies.
TL;DR: Based on 5-HT1A and5-HT7 ligand MR25003 scaffold, a new series of 1-aryl indole analogues were prepared and evaluated against 5- HT7 receptors, providing a large number of new indolic derivatives and one compound was pharmacology characterized as an antagonist.
Patent
Novel chromane compound for the treatment of pain disorders
TL;DR: In this article, the present invention relates to the compound N-[(3S)-5-(5-methoxypyrazin-2-yl)-3,4- dihydro-2H-chromen-3-yl]-6-[(2,2, 2-trifluoroethoxy)methyl]pyridine-3 carboxamide, or a pharmaceutical composition comprising said compound and to the use of said compounds in therapy
Journal ArticleDOI
Synthesis of hexahydrochromeno[4,3- b ]azepine derivatives
Gregoire Pave,Jean-Michel Léger,Christian Jarry,Marie-Claude Viaud-Massuard,Gérald Guillaumet +4 more
TL;DR: In this article, an optically pure (6a R,11a S )-7,8,9,10,11,11a-hexahydro-5-oxa-11-azacyclohepta is described via the CN( R, S ) strategy.
Journal ArticleDOI
Enantioselective synthesis of 2- and 3-substituted 2,3-dihydro[1,4]dioxino[2,3-b]pyridine derivatives and enantiomeric purity control by capillary electrophoresis.
Said Lazar,Mustapha Soukri,M. El Haddad,M. Akssira,Jean-Michel Léger,Christian Jarry,Ph. Morin,Gérald Guillaumet +7 more
TL;DR: A rapid and simple procedure for enantioselective preparation of 2- and 3-substituted 2, 3-dihydro[1,4]dioxino[2,3-b]pyridine derivatives (A and B) is described.
References
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Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.
TL;DR: The analysis described shows K I does not equal I 50 when competitive inhibition kinetics apply; however, K I is equal to I 50 under conditions of either noncompetitive or uncompetitive kinetics.
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The Palladium‐Catalyzed Cross‐Coupling Reactions of Organotin Reagents with Organic Electrophiles [New Synthetic Methods (58)]
TL;DR: The cross-coupling of organotin reagents with a variety of organic electrophiles, catalyzed by palladium, provides a novel method for generating a carbon-carbon bond.
Journal ArticleDOI
Current advances and trends in the treatment of depression
Pierre Blier,Claude de Montigny +1 more
TL;DR: A better understanding of the neurobiological basis for the delayed onset of action of antidepressant treatments has led to the elaboration of strategies that could accelerate the antidepressant response.
Journal Article
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Bryan L. Roth,S C Craigo,M S Choudhary,Ahmet Uluer,Frederick J. Monsma,Y Shen,Herbert Y. Meltzer,David R. Sibley +7 more
TL;DR: The authors examined the affinities of 36 typical and atypical antipsychotic agents for the cloned rat 5-hydroxytryptamine-6 and rat5-HT7 receptors in transiently expressed COS-7 cells or stably transfected HEK-293 cells to identify those with high affinity for the newly discovered 5-HT6 receptor.
Journal ArticleDOI
A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms.
Timothy W. Lovenberg,Bruce M. Baron,Luis de Lecea,Joseph D. Miller,Rebecca A. Prosser,Michael A. Rea,Pamela E. Foye,Margaret M. Racke,Amy L. Slone,Barry W. Siegel,Patria E. Danielson,J. Gregor Sutcliffe,Mark G. Erlander +12 more
TL;DR: The cloning and characterization of a novel serotonin receptor, designated as 5-HT7, which is coupled to the stimulation of adenylyl cyclase is reported, suggesting a physiological role in the regulation of circadian rhythms for one subtype of serotonin receptor.