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dc.contributor.author원호식-
dc.date.accessioned2019-07-18T01:58:32Z-
dc.date.available2019-07-18T01:58:32Z-
dc.date.issued2006-05-
dc.identifier.citationBIOORGANIC & MEDICINAL CHEMISTRY, v. 14, No. 9, Page. 3090-3097en_US
dc.identifier.issn0968-0896-
dc.identifier.issn1464-3391-
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S0968089605012034-
dc.identifier.urihttps://repository.hanyang.ac.kr/handle/20.500.11754/107589-
dc.description.abstractRacemate physicochemical descriptors are employed to probe the quantitative structure-activity relationship of spirosuccinimide type aldose reductase inhibitors and the in vivo inhibitory activity of sorbitol accumulation. The in vivo activity data include the percent inhibition and ED50 assay results on the literature. The derived QSAR equations show that the hydrophobic character of aldose reductase inhibitor is the major contributing factor to enhance in vivo activity. As the hydrophobicity of compounds is related to both the membrane permeability and the binding affinity to the aldose reductase, its contribution to the pharmacokinetic behavior is further scrutinized by evaluating pK(a) and the Caco-2 cell permeability. The high correlation between ED50 and the Caco-2 cell permeability of in vitro active compounds indicates that the membrane permeability is essential for in vivo efficacy. (c) 2005 Elsevier Ltd. All rights reserved.en_US
dc.language.isoen_USen_US
dc.publisherPERGAMON-ELSEVIER SCIENCE LTDen_US
dc.subjectQSARen_US
dc.subjectaldose reductase inhibitoren_US
dc.subjectsorbitol accumulationen_US
dc.subjectCaco-2 cell permeabilityen_US
dc.titleQuantitative structure-activity relationship of spirosuccinimide type aldose reductase inhibitors diminishing sorbitol accumulation in vivoen_US
dc.typeArticleen_US
dc.identifier.doi10.1016/j.bmc.2005.12.019-
dc.relation.journalBIOORGANIC & MEDICINAL CHEMISTRY-
dc.contributor.googleauthorKo, Kwangseok-
dc.contributor.googleauthorWon, Hoshik-
dc.contributor.googleauthorWon, Youngdo-
dc.relation.code2009201329-
dc.sector.campusE-
dc.sector.daehakCOLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY[E]-
dc.sector.departmentDEPARTMENT OF CHEMICAL AND MOLECULAR ENGINEERING-
dc.identifier.pidhswon-


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