Abstract
The solid-phase synthesis of a new series of 19 biomimetics of long-chain arylpiperazines, namely flexible quinoline sulfonamides of aryl(heteroaryl)oxy-/heteroarylthio-ethyl 4-aminomethylpiperidines, is reported. Various structural modifications applied followed by biological evaluation for 5-HT1A, 5-HT6, and 5-HT7 receptors gave further support of a possible replacement of arylpiperazine with aryloxy-/arylthio-ethyl derivatives of alicyclic amines and control of receptor selectivity upon diversification in the aryl(heteroaryl)oxy-/heteroarylthio-ethyl fragment.
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Drug Design
-
Ethers
-
HEK293 Cells
-
Humans
-
Molecular Structure
-
Piperidines / chemical synthesis*
-
Piperidines / chemistry
-
Piperidines / pharmacology
-
Protein Binding
-
Quinolines / chemical synthesis*
-
Quinolines / chemistry
-
Quinolines / pharmacology
-
Radioligand Assay
-
Receptor, Serotonin, 5-HT1A / genetics
-
Receptor, Serotonin, 5-HT1A / metabolism*
-
Receptors, Serotonin / genetics
-
Receptors, Serotonin / metabolism*
-
Solid-Phase Synthesis Techniques
-
Structure-Activity Relationship
-
Sulfonamides / chemical synthesis*
-
Sulfonamides / chemistry
-
Sulfonamides / pharmacology
-
Transfection
Substances
-
Ethers
-
Piperidines
-
Quinolines
-
Receptors, Serotonin
-
Sulfonamides
-
serotonin 7 receptor
-
Receptor, Serotonin, 5-HT1A