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dc.contributor.authorGuo, Kai
dc.contributor.authorMutter, Roger
dc.contributor.authorHeal, William
dc.contributor.authorReddy, Tummala Rama Krishna
dc.contributor.authorCope, Hannah
dc.contributor.authorPratt, Steven
dc.contributor.authorThompson, Mark J.
dc.contributor.authorChen, Beining
dc.date.accessioned2013-01-11T14:59:13Z
dc.date.available2013-01-11T14:59:13Z
dc.date.issued2008
dc.identifier.citationGuo , K , Mutter , R , Heal , W , Reddy , T R K , Cope , H , Pratt , S , Thompson , M J & Chen , B 2008 , ' Synthesis and Evaluation of a Focused Library of Pyridine Dicarbonitriles Against Prion Disease ' , European Journal of Medicinal Chemistry , vol. 43 , no. 1 , pp. 93-106 . https://doi.org/10.1016/j.ejmech.2007.02.018
dc.identifier.issn1768-3254
dc.identifier.otherPURE: 1374937
dc.identifier.otherPURE UUID: a20aa976-e625-4c07-a37d-5ef8b735e2c4
dc.identifier.otherScopus: 38349054600
dc.identifier.urihttp://hdl.handle.net/2299/9593
dc.description.abstractWe report the preparation and screening of a set of 55 pyridine dicarbonitriles as potential prion disease therapeutics. Use of microwave irradiation in an attempt to improve the synthesis typically led to only small enhancement in yields but gave cleaner reactions facilitating product isolation. The library was analysed for binding to human prion protein (huPrPC) by surface plasmon resonance and for inhibition of the formation of its partially protease resistant isoform PrPSc in mouse brain cells (SMB). A total of 26 compounds were found to bind to huPrPC whilst 12 showed discernable inhibition of PrPSc formation, five displaying EC50s in the range 2.5e9 mM. Two compounds were found to reduce PrPSc levels to below 30% relative to an untreated control at 50 nM.en
dc.language.isoeng
dc.relation.ispartofEuropean Journal of Medicinal Chemistry
dc.titleSynthesis and Evaluation of a Focused Library of Pyridine Dicarbonitriles Against Prion Diseaseen
dc.contributor.institutionDepartment of Pharmacy
dc.contributor.institutionSchool of Life and Medical Sciences
dc.contributor.institutionHealth & Human Sciences Research Institute
dc.contributor.institutionMedicinal and Analytical Chemistry
dc.description.statusPeer reviewed
dc.identifier.urlhttp://www.sciencedirect.com/science/article/pii/S0223523407001158
rioxxterms.versionVoR
rioxxterms.versionofrecordhttps://doi.org/10.1016/j.ejmech.2007.02.018
rioxxterms.typeJournal Article/Review
herts.preservation.rarelyaccessedtrue


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