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 ligands. Affinities and intrinsic activities for the human cloned mt1 and MT2 receptors were examined and compared with those of some 2-substituted melatonin derivatives recently described by us. A quantitative structure activity relationship (QSAR) study of the sixteen 2-substituted indole compounds, 5a-k, 1, 8-11, using partial least squares (PLS) and multiple regression analysis (MRA) revealed the existence of an optimal range of lipophilicity for the C2 indole substituent. There are also indications that planar, electron-withdrawing substituents contribute to the affin...
Molecular superposition models guided the design of novel melatonin receptor ligands characterized b...
Since melatonin (MLT) was discovered, several physio-pathological functions have been associated wit...
The known neuroprotective actions of melatonin could be due to its antioxidant or radical scavenging...
Several indole analogues of melatonin (MLT) were obtained by moving the MLT side chain from C(3) to ...
The design, synthesis, and biological profile of several indole melatonin analogues with a conformat...
The synthesis of several novel indole melatonin analogues substituted at the 2-position with acylami...
A novel series of melatonin receptor ligands was discovered by opening the cyclic scaffolds of known...
The three-dimensional quantitative structure-activity relationship comparative molecular field analy...
Three-dimensional homology models of human MT1 and MT2 melatonin receptors were built with the aim ...
Die vorliegende Arbeit befasst sich mit der Synthese von Liganden der Melatonin-Rezeptoren (MR). Die...
The work contained in this thesis forms part of an ongoing programme to examine the structure of the...
The three-dimensional quantitative structure-activity relationship comparative molecular field analy...
Three-dimensional homology models of human MT1 and MT2 melatonin receptors were built with the aim ...
A novel series of melatonin receptor ligands was discovered by opening the cyclic scaffolds of known...
This work reports the design and synthesis of novel alkylamides, characterized by a dibenzo- [a,d]c...
Molecular superposition models guided the design of novel melatonin receptor ligands characterized b...
Since melatonin (MLT) was discovered, several physio-pathological functions have been associated wit...
The known neuroprotective actions of melatonin could be due to its antioxidant or radical scavenging...
Several indole analogues of melatonin (MLT) were obtained by moving the MLT side chain from C(3) to ...
The design, synthesis, and biological profile of several indole melatonin analogues with a conformat...
The synthesis of several novel indole melatonin analogues substituted at the 2-position with acylami...
A novel series of melatonin receptor ligands was discovered by opening the cyclic scaffolds of known...
The three-dimensional quantitative structure-activity relationship comparative molecular field analy...
Three-dimensional homology models of human MT1 and MT2 melatonin receptors were built with the aim ...
Die vorliegende Arbeit befasst sich mit der Synthese von Liganden der Melatonin-Rezeptoren (MR). Die...
The work contained in this thesis forms part of an ongoing programme to examine the structure of the...
The three-dimensional quantitative structure-activity relationship comparative molecular field analy...
Three-dimensional homology models of human MT1 and MT2 melatonin receptors were built with the aim ...
A novel series of melatonin receptor ligands was discovered by opening the cyclic scaffolds of known...
This work reports the design and synthesis of novel alkylamides, characterized by a dibenzo- [a,d]c...
Molecular superposition models guided the design of novel melatonin receptor ligands characterized b...
Since melatonin (MLT) was discovered, several physio-pathological functions have been associated wit...
The known neuroprotective actions of melatonin could be due to its antioxidant or radical scavenging...