Identification of Optically Active Pyrimidine Derivatives as Selective 5-HT 2C Modulators

A series of pyrimidine derivatives - were synthesized and evaluated for their binding affinities towards 5-HT receptors. With regard to designed molecules - , the influence of the size of alkyl ether and the absolute configuration of a stereogenic center on the 5-HT binding affinity and selectivity...

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Veröffentlicht in:	Molecules (Basel, Switzerland) Switzerland), 2017-08, Vol.22 (9)
Hauptverfasser:	Kim, Juhyeon, Jo, Hanbyeol, Lee, Hyunseung, Choo, Hyunah, Kim, Hak Joong, Pae, Ae Nim, Cho, Yong Seo, Min, Sun-Joon
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals CHO Cells Cricetulus Models, Molecular Molecular Structure Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Receptor, Serotonin, 5-HT2C - metabolism Serotonin 5-HT2 Receptor Agonists - chemical synthesis Serotonin 5-HT2 Receptor Agonists - chemistry Serotonin 5-HT2 Receptor Agonists - pharmacology Structure-Activity Relationship
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container_title	Molecules (Basel, Switzerland)
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creator	Kim, Juhyeon Jo, Hanbyeol Lee, Hyunseung Choo, Hyunah Kim, Hak Joong Pae, Ae Nim Cho, Yong Seo Min, Sun-Joon
description	A series of pyrimidine derivatives - were synthesized and evaluated for their binding affinities towards 5-HT receptors. With regard to designed molecules - , the influence of the size of alkyl ether and the absolute configuration of a stereogenic center on the 5-HT binding affinity and selectivity was studied. The most promising diasteromeric mixtures and were selected in the initial radioligand binding assay and they were further synthesized as optically active forms starting from optically active alcohols and , prepared by an enzymatic kinetic resolution. Pyrimidine analogue ( )- displayed an excellent 5-HT binding affinity with good selectivity values against a broad range of other 5-HT receptor subtypes.
doi_str_mv	10.3390/molecules22091416
format	Article
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source	MDPI - Multidisciplinary Digital Publishing Institute; MEDLINE; DOAJ Directory of Open Access Journals; EZB-FREE-00999 freely available EZB journals; PubMed Central; Free Full-Text Journals in Chemistry
subjects	Animals CHO Cells Cricetulus Models, Molecular Molecular Structure Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Receptor, Serotonin, 5-HT2C - metabolism Serotonin 5-HT2 Receptor Agonists - chemical synthesis Serotonin 5-HT2 Receptor Agonists - chemistry Serotonin 5-HT2 Receptor Agonists - pharmacology Structure-Activity Relationship
title	Identification of Optically Active Pyrimidine Derivatives as Selective 5-HT 2C Modulators
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