000824107 001__ 824107
000824107 005__ 20220930130111.0
000824107 0247_ $$2doi$$a10.3390/molecules21091160
000824107 0247_ $$2Handle$$a2128/13129
000824107 0247_ $$2WOS$$aWOS:000385479800057
000824107 0247_ $$2altmetric$$aaltmetric:21831540
000824107 0247_ $$2pmid$$a27598109
000824107 037__ $$aFZJ-2016-06731
000824107 082__ $$a540
000824107 1001_ $$0P:(DE-Juel1)145778$$aDrerup, Christian$$b0
000824107 245__ $$aSynthesis of a Potent Aminopyridine-Based nNOS-Inhibitor by Two Recent No-Carrier-Added $^{18}$F-Labelling Methods
000824107 260__ $$aBasel$$bMDPI75390$$c2016
000824107 3367_ $$2DRIVER$$aarticle
000824107 3367_ $$2DataCite$$aOutput Types/Journal article
000824107 3367_ $$0PUB:(DE-HGF)16$$2PUB:(DE-HGF)$$aJournal Article$$bjournal$$mjournal$$s1480951209_8031
000824107 3367_ $$2BibTeX$$aARTICLE
000824107 3367_ $$2ORCID$$aJOURNAL_ARTICLE
000824107 3367_ $$00$$2EndNote$$aJournal Article
000824107 520__ $$aNitric oxide (NO), an important multifunctional signaling molecule, is produced by threeisoforms of NO-synthase (NOS) and has been associated with neurodegenerative disorders. Selectiveinhibitors of the subtypes iNOS (inducible) or nNOS (neuronal) are of great interest for decodingneurodestructive key factors, and 18F-labelled analogues would allow investigating the NOS-functionby molecular imaging with positron emission tomography. Especially, the highly selective nNOSinhibitor 6-((3-((3-fluorophenethylamino)methyl)phenoxy)methyl)-4-methylpyridin-2-amine (10)lends itself as suitable compound to be 18F-labelled in no-carrier-added (n.c.a.) form. For preparationof the 18F-labelled nNOS-Inhibitor [18F]10 a “build-up” radiosynthesis was developed based on acorresponding iodonium ylide as labelling precursor. The such activated phenethyl group of thecompound was efficiently and regioselectively labelled with n.c.a. [18F]fluoride in 79% radiochemicalyield (RCY). After conversion by reductive amination and microwave assisted displacement of theprotecting groups, the desired nNOS-inhibitor was obtained in about 15% total RCY. Alternatively,for a simplified “late-stage” 18F-labelling procedure a corresponding boronic ester precursor wassynthesized and successfully used in a newer, copper(II) mediated n.c.a. 18F-fluoro-deboroniationreaction, achieving the same total RCY. Thus, both methods proved comparatively suited to providethe highly selective NOS-inhibitor [18F]10 as probe for preclinical in vivo studies.
000824107 536__ $$0G:(DE-HGF)POF3-573$$a573 - Neuroimaging (POF3-573)$$cPOF3-573$$fPOF III$$x0
000824107 588__ $$aDataset connected to CrossRef
000824107 7001_ $$0P:(DE-Juel1)131818$$aErmert, Johannes$$b1$$eCorresponding author$$ufzj
000824107 7001_ $$0P:(DE-Juel1)131816$$aCoenen, Heinrich Hubert$$b2$$ufzj
000824107 773__ $$0PERI:(DE-600)2008644-1$$a10.3390/molecules21091160$$gVol. 21, no. 9, p. 1160 -$$n9$$p1160 -$$tMolecules$$v21$$x1420-3049$$y2016
000824107 8564_ $$uhttps://juser.fz-juelich.de/record/824107/files/molecules-21-01160.pdf$$yOpenAccess
000824107 8564_ $$uhttps://juser.fz-juelich.de/record/824107/files/molecules-21-01160.gif?subformat=icon$$xicon$$yOpenAccess
000824107 8564_ $$uhttps://juser.fz-juelich.de/record/824107/files/molecules-21-01160.jpg?subformat=icon-1440$$xicon-1440$$yOpenAccess
000824107 8564_ $$uhttps://juser.fz-juelich.de/record/824107/files/molecules-21-01160.jpg?subformat=icon-180$$xicon-180$$yOpenAccess
000824107 8564_ $$uhttps://juser.fz-juelich.de/record/824107/files/molecules-21-01160.jpg?subformat=icon-640$$xicon-640$$yOpenAccess
000824107 8564_ $$uhttps://juser.fz-juelich.de/record/824107/files/molecules-21-01160.pdf?subformat=pdfa$$xpdfa$$yOpenAccess
000824107 8767_ $$8molecules-146561$$92016-08-26$$d2016-08-26$$eAPC$$jZahlung erfolgt$$pmolecules-146561$$zCHF 1530,-
000824107 909CO $$ooai:juser.fz-juelich.de:824107$$popenCost$$pVDB$$pdriver$$pOpenAPC$$popen_access$$popenaire$$pdnbdelivery
000824107 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)131818$$aForschungszentrum Jülich$$b1$$kFZJ
000824107 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)131816$$aForschungszentrum Jülich$$b2$$kFZJ
000824107 9131_ $$0G:(DE-HGF)POF3-573$$1G:(DE-HGF)POF3-570$$2G:(DE-HGF)POF3-500$$3G:(DE-HGF)POF3$$4G:(DE-HGF)POF$$aDE-HGF$$bKey Technologies$$lDecoding the Human Brain$$vNeuroimaging$$x0
000824107 9141_ $$y2016
000824107 915__ $$0StatID:(DE-HGF)0200$$2StatID$$aDBCoverage$$bSCOPUS
000824107 915__ $$0LIC:(DE-HGF)CCBY4$$2HGFVOC$$aCreative Commons Attribution CC BY 4.0
000824107 915__ $$0StatID:(DE-HGF)0600$$2StatID$$aDBCoverage$$bEbsco Academic Search
000824107 915__ $$0StatID:(DE-HGF)0100$$2StatID$$aJCR$$bMOLECULES : 2015
000824107 915__ $$0StatID:(DE-HGF)0501$$2StatID$$aDBCoverage$$bDOAJ Seal
000824107 915__ $$0StatID:(DE-HGF)0500$$2StatID$$aDBCoverage$$bDOAJ
000824107 915__ $$0StatID:(DE-HGF)0111$$2StatID$$aWoS$$bScience Citation Index Expanded
000824107 915__ $$0StatID:(DE-HGF)0150$$2StatID$$aDBCoverage$$bWeb of Science Core Collection
000824107 915__ $$0StatID:(DE-HGF)9900$$2StatID$$aIF < 5
000824107 915__ $$0StatID:(DE-HGF)0510$$2StatID$$aOpenAccess
000824107 915__ $$0StatID:(DE-HGF)0030$$2StatID$$aPeer Review$$bASC
000824107 915__ $$0StatID:(DE-HGF)1150$$2StatID$$aDBCoverage$$bCurrent Contents - Physical, Chemical and Earth Sciences
000824107 915__ $$0StatID:(DE-HGF)0310$$2StatID$$aDBCoverage$$bNCBI Molecular Biology Database
000824107 915__ $$0StatID:(DE-HGF)0300$$2StatID$$aDBCoverage$$bMedline
000824107 915__ $$0StatID:(DE-HGF)0199$$2StatID$$aDBCoverage$$bThomson Reuters Master Journal List
000824107 920__ $$lyes
000824107 9201_ $$0I:(DE-Juel1)INM-5-20090406$$kINM-5$$lNuklearchemie$$x0
000824107 980__ $$ajournal
000824107 980__ $$aVDB
000824107 980__ $$aUNRESTRICTED
000824107 980__ $$aI:(DE-Juel1)INM-5-20090406
000824107 9801_ $$aFullTexts
000824107 980__ $$aAPC