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 …
MT1‐Selective Melatonin Receptor Ligands: Synthesis, Pharmacological Evaluation, and Molecular Dynamics Investigation of N‐{[(3‐O‐Substituted)anilino]alkyl} …
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 …
owing to the limited knowledge of the structural features conferring selectivity for the MT1 …
Design and Synthesis of N-(3,3-Diphenylpropenyl)alkanamides as a Novel Class of High-Affinity MT2-Selective Melatonin Receptor Ligands
A novel series of melatonin receptor ligands was discovered by opening the cyclic scaffolds
of known classes of high affinity melatonin receptor antagonists, while retaining the …
of known classes of high affinity melatonin receptor antagonists, while retaining the …
N-(Substituted-anilinoethyl)amides: Design, Synthesis, and Pharmacological Characterization of a New Class of Melatonin Receptor Ligands
A novel series of melatonin receptor ligands, characterized by a N-(substituted-anilinoethyl)
amido scaffold, along with preliminary structure–activity relationships (SARs), is presented …
amido scaffold, along with preliminary structure–activity relationships (SARs), is presented …
Bivalent ligand approach on N-{2-[(3-methoxyphenyl) methylamino] ethyl} acetamide: Synthesis, binding affinity and intrinsic activity for MT1 and MT2 melatonin …
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 …
receptors of new dimeric melatonin receptor ligands in which two units of the monomeric …
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 …
[a, d] cycloheptene nucleus, as melatonin (MLT) receptor ligands. The tricyclic scaffold 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 …
Analysis of Structure−Activity Relationships for MT2 Selective Antagonists by Melatonin MT1 and MT2 Receptor Models
Three-dimensional homology models of human MT1 and MT2 melatonin receptors were
built with the aim to investigate the structure− activity relationships (SARs) of MT2 selective …
built with the aim to investigate the structure− activity relationships (SARs) of MT2 selective …
Tetrahydroquinoline ring as a versatile bioisostere of tetralin for melatonin receptor ligands
A new family of melatonin receptor ligands, characterized by a tetrahydroquinoline (THQ)
scaffold carrying an amide chain in position 3, was devised as conformationally constrained …
scaffold carrying an amide chain in position 3, was devised as conformationally constrained …
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 …