title: Quinolinesulfonamides of aryloxy-/arylthio-ethyl piperidines: influence of an arylether fragment on 5-HT1A/5-HT7 receptor selectivity.
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.
authors: Department of Medicinal Chemistry, Jagiellonian University Medical College, Kraków, Poland.
authors: Katarzyna
authors: K
authors: Grychowska
authors: Krzysztof
authors: K
authors: Marciniec
authors: Vittorio
authors: V
authors: Canale
authors: Michał
authors: M
authors: Szymiec
authors: Grzegorz
authors: G
authors: Glanowski
authors: Grzegorz
authors: G
authors: Satała
authors: Andrzej
authors: A
authors: Maślankiewicz
authors: Maciej
authors: M
authors: Pawłowski
authors: Andrzej J
authors: AJ
authors: Bojarski
authors: Paweł
authors: P
authors: Zajdel
mesh_terms: D015195:Drug Design; D004987:Ethers; D057809:HEK293 Cells; D006801:Humans; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011485:Protein Binding; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D044282:Receptor, Serotonin, 5-HT1A / Q000235:genetics / Q000378:metabolism*; D011985:Receptors, Serotonin / Q000235:genetics / Q000378:metabolism*; D060327:Solid-Phase Synthesis Techniques; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014162:Transfection
chemical_list: D004987:Ethers; D010880:Piperidines; D011804:Quinolines; D011985:Receptors, Serotonin; D013449:Sulfonamides; C104425:serotonin 7 receptor; D044282:Receptor, Serotonin, 5-HT1A