[HTML][HTML] Synthesis and Functional Characterization of Substituted Isoquinolinones as MT2-Selective Melatoninergic Ligands
Y Hu, KH Chan, X He, MKC Ho, YH Wong - Plos one, 2014 - journals.plos.org
A series of substituted isoquinolinones were synthesized and their binding affinities and
functional activities towards human melatonin MT1 and MT2 receptors were evaluated …
functional activities towards human melatonin MT1 and MT2 receptors were evaluated …
Molecular basis defining the selectivity of substituted isoquinolinones for the melatonin MT2 receptor
Melatonin MT 1 and MT 2 receptors represent attractive drug targets for the treatment of
various disorders. However, the high conservation of the melatonin binding pocket has …
various disorders. However, the high conservation of the melatonin binding pocket has …
Highly Potent and Selective MT2 Melatonin Receptor Full Agonists from Conformational Analysis of 1-Benzyl-2-acylaminomethyl-tetrahydroquinolines
Molecular superposition models guided the design of novel melatonin receptor ligands
characterized by a 2-acylaminomethyltetrahydroquinoline scaffold. Starting from the …
characterized by a 2-acylaminomethyltetrahydroquinoline scaffold. Starting from the …
Synthesis and pharmacological evaluation of 1, 2, 3, 4-tetrahydropyrazino [1, 2-a] indole and 2-[(phenylmethylamino) methyl]-1H-indole analogues as novel …
C Markl, MI Attia, J Julius, S Sethi… - Bioorganic & medicinal …, 2009 - Elsevier
Two novel series of melatonin-derived compounds have been synthesized and
pharmacologically evaluated at the MT1 and MT2 subtypes of melatonin receptors …
pharmacologically evaluated at the MT1 and MT2 subtypes of melatonin receptors …
Synthesis, pharmacological characterization and QSAR studies on 2-substituted indole melatonin receptor ligands
A number of 6-methoxy-1-(2-propionylaminoethyl) indoles, carrying properly selected
substituents at the C-2 indole position, were prepared and tested as melatonin receptor …
substituents at the C-2 indole position, were prepared and tested as melatonin receptor …
Synthesis and pharmacological evaluation of pentacyclic 6a, 7-dihydrodiindole and 2, 3-dihydrodiindole derivatives as novel melatoninergic ligands
MI Attia, PA Witt-Enderby, J Julius - Bioorganic & medicinal chemistry, 2008 - Elsevier
The synthesis of novel melatonin analogues 3a and 4a–c designed as melatonin receptor
ligands is described. Among the newly synthesized ligands, 2-((S)-2-hydroxymethylindolin-1 …
ligands is described. Among the newly synthesized ligands, 2-((S)-2-hydroxymethylindolin-1 …
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 …
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 …
amide derivatives were synthesized and evaluated as melatonin receptor ligands. The …
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 …
melatoninergic ligands. Binding affinity assays were performed on cloned human MT1 and …
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 …
processes, including the circadian rhythm and seasonal adaptation. The two subtypes of …