Design and synthesis of 3-phenyl tetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands

S Yous, S Durieux-Poissonnier, E Lipka-Belloli… - Bioorganic & medicinal …, 2003 - Elsevier
Tetrahydronaphthalenic analogues of melatonin have been synthesized and evaluated as
melatonin receptor ligands. Introduction of a phenyl substituent in the 3-position of the …

Synthesis of 3-phenylnaphthalenic derivatives as new selective MT2 melatoninergic ligands

S Poissonnier-Durieux, M Ettaoussi, B Pérès… - Bioorganic & medicinal …, 2008 - Elsevier
A series of naphthalenic analogues of melatonin were prepared and evaluated as melatonin
receptor MT2 selective ligands. Activity and MT2 selectivity can be modulated with suitable …

Design and synthesis of 3-phenyltetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands. Part II

S Durieux, A Chanu, C Bochu, V Audinot… - Bioorganic & medicinal …, 2009 - Elsevier
Following our studies of the melatoninergic receptors, we have developed new
tetrahydronaphthalenic derivatives of melatonin that have been tested as selective …

Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT1 melatoninergic ligands

C Mésangeau, B Pérès, C Descamps-François… - Bioorganic & Medicinal …, 2010 - Elsevier
Novel heterodimer analogues of melatonin were synthesized, when agomelatine (1) and
various aryl units are linked via a linear alkyl chain through the methoxy group. The …

Design and synthesis of naphthalenic derivatives as new ligands at the melatonin binding site MT3

V Leclerc, M Ettaoussi, M Rami, A Farce… - European journal of …, 2011 - Elsevier
Naphthalenic analogs of MCA-NAT (5-methoxycarbonylamino-N-acetyltryptamine) have
been synthesized and evaluated as melatonin receptor ligands. Introduction of a …

Heterocyclic aminopyrrolidine derivatives as melatoninergic agents

LQ Sun, J Chen, RJ Mattson, JR Epperson… - Bioorganic & medicinal …, 2003 - Elsevier
A series of chiral heterocyclic aminopyrrolidine derivatives was synthesized as novel
melatoninergic ligands. Binding affinity assays were performed on cloned human MT1 and …

Synthesis of substituted N-[3-(3-methoxyphenyl) propyl] amides as highly potent MT2-selective melatonin ligands

Y Hu, MKC Ho, KH Chan, DC New, YH Wong - Bioorganic & Medicinal …, 2010 - Elsevier
A series of substituted N-[3-(3-methoxyphenyl) propyl] amides were synthesized and their
binding affinities towards human melatonin MT1 and MT2 receptors were evaluated. It was …

Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity

V Lucini, M Pannacci, F Scaglione… - Journal of medicinal …, 2004 - ACS Publications
This work reports the design and synthesis of novel alkylamides, characterized by a dibenzo
[a, d] cycloheptene nucleus, as melatonin (MLT) receptor ligands. The tricyclic scaffold was …

Towards the Development of Mixed MT1‐Agonist/MT2‐Antagonist Melatonin Receptor Ligands

G Spadoni, A Bedini, T Guidi, G Tarzia… - ChemMedChem …, 2006 - Wiley Online Library
Herein we report attempts to optimize the pharmacological properties of 5‐(2‐
hydroxyethoxy)‐N‐acetyltryptamine (5‐HEAT), a melatonin receptor ligand previously …

2-[(2,3-Dihydro-1H-indol-1-yl)methyl]melatonin Analogues: A Novel Class of MT2-Selective Melatonin Receptor Antagonists

DP Zlotos, MI Attia, J Julius, S Sethi… - Journal of medicinal …, 2009 - ACS Publications
A novel series of 2-[(2, 3-dihydro-1 H-indol-1-yl) methyl] melatonin analogues has been
prepared to probe the steric and electronic properties of the binding pocket of the MT2 …