ChemInform Abstract: 5-(4-Hydroxy-6-methyl-2-oxo-2H-pyran-3-yl) -7-phenyl-2,3,6,7-tetrahydro-1,4-thiazepines as Compounds with High Affinity at the Benzodiazepine Binding Site on GABAA Receptors

Autor:	K Heinecke, C Kronbach, K Unverferth, R Dieckmann, C Grunwald, R. Schindler, U Egerland, N Höfgen
Rok vydání:	2011
Předmět:	chemistry.chemical_compound chemistry Stereochemistry Pyran Hydrogen bond GABAA receptor Thiazepine Structure–activity relationship Stereoisomerism General Medicine Pharmacophore Selectivity
Zdroj:	ChemInform. 42
ISSN:	0931-7597
DOI:	10.1002/chin.201125210
Popis:	A series of thiazepines has been studied as new ligands for the benzodiazepine binding site of the GABAA receptor. Compounds with high affinity and weak selectivity regarding alpha beta3gamma2, alpha2beta3gamma2, alpha3beta3gamma2, and alpha5beta3gamma2 subtypes were found. The pharmacophore is discussed based on experimental and theoretical results. The thiazepine sulfur atom was found to be able to act as hydrogen bond acceptor.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::3549edfacb73f8d46ed4a2d4ceefa7c4 https://doi.org/10.1002/chin.201125210 Zobrazit plný text záznamu Plný text