Search results for "HEXAHYDROCYCLOPENTAISOQUINOLINES"

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Dopaminergic isoquinolines with hexahydrocyclopenta[ ij ]-isoquinolines as D 2 -like selective ligands

2016

Dopamine receptors (DR) ligands are potential drug candidates for treating neurological disorders including schizophrenia or Parkinson's disease. Three series of isoquinolines: (E)-1-styryl-1,2,3,4-tetrahydroisoquinolines (series 1), 7-phenyl-1,2,3,7,8,8a-hexahydrocyclopenta[ij]-IQs (HCPIQs) (series 2) and (E)-1-(prop-1-en-1-yl)-1,2,3,4- tetrahydroisoquinolines (series 3), were prepared to determine their affinity for both D1and D2-like DR. The effect of different substituents on the nitrogen atom (methyl or allyl), the dioxygenated function (methoxyl or catechol), the substituent at the β-position of the THIQ skeleton, and the presence or absence of the cyclopentane motif, were studied. We…

Models MolecularMolecular modelProtein ConformationStereochemistryDopamine AgentsSubstituentCyclopentanesLigands010402 general chemistry01 natural sciencesSubstrate SpecificityStructure-Activity Relationshipchemistry.chemical_compoundDrug DiscoveryHuman Umbilical Vein Endothelial CellsmedicineHumansStructure–activity relationshipCYTOTOXICITYMOLECULAR MODELINGCyclopentaneSTRUCTURE-ACTIVITY RELATIONSHIPSTETRAHYDROISOQUINOLINESPharmacologyCatecholReceptors Dopamine D2010405 organic chemistryOtras Ciencias QuímicasOrganic ChemistryDopaminergicCiencias QuímicasGeneral MedicineIsoquinolines0104 chemical sciencesOxygenDOPAMINERGICchemistryTHIQHEXAHYDROCYCLOPENTAISOQUINOLINESSelectivityCIENCIAS NATURALES Y EXACTASmedicine.drugEuropean Journal of Medicinal Chemistry
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