Development of substituted N-[3-(3-methoxylphenyl) propyl] amides as MT2-selective melatonin agonists: Improving metabolic stability

Y Hu, J Zhu, KH Chan, YH Wong - Bioorganic & medicinal chemistry, 2013 - Elsevier
A series of novel and selective N-[3-(6-benzyloxy-3-methoxyphenyl) propyl] amides has
recently been shown to possess sub-nanomolar range binding affinity to the type 2 …

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 …

Synthesis and Structure−Affinity−Activity Relationships of Novel Benzofuran Derivatives as MT2 Melatonin Receptor Selective Ligands

V Wallez, S Durieux-Poissonnier… - Journal of medicinal …, 2002 - ACS Publications
A series of N-(2-phenylbenzofuran-3-yl) ethyl amide and N-(2-arylalkylbenzofuran-3-yl) ethyl
amide derivatives were synthesized and evaluated as melatonin receptor ligands. The …

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 …

MT1‐Selective Melatonin Receptor Ligands: Synthesis, Pharmacological Evaluation, and Molecular Dynamics Investigation of N‐{[(3‐O‐Substituted)anilino]alkyl} …

S Rivara, D Pala, A Lodola, M Mor, V Lucini… - …, 2012 - Wiley Online Library
The design of compounds selective for the MT1 melatonin receptor is still a challenging task
owing to the limited knowledge of the structural features conferring selectivity for the MT1 …

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 …

N-{2-[2-(4-Phenylbutyl) benzofuran-4-yl] cyclopropylmethyl} acetamide: an orally bioavailable melatonin receptor agonist

LQ Sun, K Takaki, J Chen, L Iben, JO Knipe… - Bioorganic & medicinal …, 2004 - Elsevier
N-{2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl}acetamide: an orally bioavailable
melatonin receptor agonist - ScienceDirect Skip to main contentSkip to article Elsevier logo …

Bivalent ligand approach on N-{2-[(3-methoxyphenyl) methylamino] ethyl} acetamide: Synthesis, binding affinity and intrinsic activity for MT1 and MT2 melatonin …

G Spadoni, A Bedini, P Orlando, S Lucarini… - Bioorganic & medicinal …, 2011 - Elsevier
We report the synthesis, binding properties and intrinsic activity at MT1 and MT2 melatonin
receptors of new dimeric melatonin receptor ligands in which two units of the monomeric …

Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands

G Li, H Zhou, Y Jiang, H Keim, SW Topiol… - Bioorganic & medicinal …, 2011 - Elsevier
Two series of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide
derivatives exhibiting diverse functionality at rat MT1 and MT2 receptors are reported …

Characterization of substituted phenylpropylamides as highly selective agonists at the melatonin MT2 receptor

KH Chan, Y Hu, M KC Ho… - Current Medicinal …, 2013 - ingentaconnect.com
Melatonin is a widely distributed hormone that regulates several major physiological
processes, including the circadian rhythm and seasonal adaptation. The two subtypes of …