{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,5]],"date-time":"2026-10-05T23:57:03Z","timestamp":1791244623578,"version":"4.1.0"},"reference-count":54,"publisher":"Radiation Research Society","issue":"5","content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Radiation Research"],"published-print":{"date-parts":[[2025,3,24]]},"abstract":"<jats:p>This research details the synthesis, structure-activity evaluation, and analysis of novel oxadiazole-based compounds for visualizing b-amyloid (Ab) in Alzheimer's disease (AD). The derivatives exhibited binding affinities to Ab aggregates in vitro. The [18F]-labeled compounds, [18F]4-(5-(4-Fluorophenyl)-1,3,4-oxadiazol-2-yl)-N, N-dimethylaniline (compound [18F] 3) and [18F] 4-(5-(4-Fluorophenyl)-1,3,4-oxadiazol-2-yl)-N-methyl-aniline (compound [18F]4), effectively labeled Ab plaques in brain sections from Alzheimer's disease patients and APP\/PS1 mice. In dynamic positron emission tomography (PET) studies on healthy mice, these compounds demonstrated favorable brain uptake followed by clearance. Additional structural alterations to compounds [18F] 3 and [18F] 4 may lead to the development of more efficient PET tracers for precise visualization of Ab plaques.<\/jats:p>","DOI":"10.1667\/rade-25-00035.1","type":"journal-article","created":{"date-parts":[[2025,3,23]],"date-time":"2025-03-23T20:02:01Z","timestamp":1742760121000},"page":"357-365","source":"Crossref","is-referenced-by-count":0,"title":["Synthesis and Evaluation of Novel 18F-labeled Oxadiazole-based Positron Emission Tomography Tracers for \u03b2-Amyloid"],"prefix":"10.1667","volume":"203","author":[{"given":"Zhongyuan","family":"Qi","sequence":"first","affiliation":[{"name":"Department of Radiology and Nuclear Medicine, Xuanwu Hospital, Capital Medical University, 00053 Beijing, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wantong","family":"Guo","sequence":"additional","affiliation":[{"name":"Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, 100875 Beijing, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mengchao","family":"Cui","sequence":"additional","affiliation":[{"name":"Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, 100875 Beijing, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jie","family":"Lu","sequence":"additional","affiliation":[{"name":"Department of Radiology and Nuclear Medicine, Xuanwu Hospital, Capital Medical University, 00053 Beijing, China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1243","reference":[{"key":"2","doi-asserted-by":"crossref","unstructured":"Z Breijyeh  and R Karaman  \"Molecules.\"  25, \"Comprehensive review on Alzheimer's disease: Causes and treatment.\" (2020)","DOI":"10.3390\/molecules25245789"},{"key":"3","doi-asserted-by":"crossref","unstructured":"X Zhou, Y Liu, Z Wu, et al.  \"Epilepsy Behav.\"  157, \"Alzheimer's disease and epilepsy: Research hotspots for comorbidity in the era of global aging.\" 109849 (2024)","DOI":"10.1016\/j.yebeh.2024.109849"},{"key":"4","doi-asserted-by":"crossref","unstructured":"DJ. Selkoe,  \"Ann N Y Acad Sci.\"  924, \"Toward a comprehensive theory for Alzheimer's disease. Hypothesis: Alzheimer's disease is caused by the cerebral accumulation and cytotoxicity of amyloid beta-protein.\" 17 (2000)","DOI":"10.1111\/j.1749-6632.2000.tb05554.x"},{"key":"5","doi-asserted-by":"crossref","unstructured":"A Pichet Binette, C Gaiteri, M Wennstrom, et al.  \"Nat Neurosci.\"  27, \"Proteomic changes in Alzheimer's disease associated with progressive Abeta plaque and tau tangle pathologies.\" 1880 (2024)","DOI":"10.1038\/s41593-024-01737-w"},{"key":"6","doi-asserted-by":"crossref","unstructured":"K Hsiao, P Chapman, S Nilsen, et al.  \"Science.\"  274, \"Correlative memory deficits, Abeta elevation, and amyloid plaques in transgenic mice.\" 99 (1996)","DOI":"10.1126\/science.274.5284.99"},{"key":"7","doi-asserted-by":"crossref","unstructured":"DR Thal, E Capetillo-Zarate, K Del Tredici, et al.  \"Sci Aging Knowledge Environ.\"  2006, \"The development of amyloid beta protein deposits in the aged brain.\" re1 (2006)","DOI":"10.1126\/sageke.2006.6.re1"},{"key":"8","doi-asserted-by":"crossref","unstructured":"T Wisniewski, J Ghiso, B Frangione,  \"Biochem Biophys Res Commun.\"  179, \"Peptides homologous to the amyloid protein of Alzheimer's disease containing a glutamine for glutamic acid substitution have accelerated amyloid fibril formation.\" 1247 (1991)","DOI":"10.1016\/0006-291X(91)91706-I"},{"key":"9","doi-asserted-by":"crossref","unstructured":"C Cheignon, M Tomas, D Bonnefont-Rousselot, et al.  \"Redox Biol.\"  14, \"Oxidative stress and the amyloid beta peptide in Alzheimer's disease.\" 450 (2018)","DOI":"10.1016\/j.redox.2017.10.014"},{"key":"10","unstructured":"WJ Jansen, R Ossenkoppele, DL Knol, et al.  \"JAMA.\"  313, \"Prevalence of cerebral amyloid pathology in persons without dementia: a meta-analysis.\" 1924 (2015)"},{"key":"11","doi-asserted-by":"crossref","unstructured":"AG Vlassenko, TL Benzinger, JC Morris,  \"Biochim Biophys Acta.\"  1822, \"PET amyloid-beta imaging in preclinical Alzheimer's disease.\" 370 (2012)","DOI":"10.1016\/j.bbadis.2011.11.005"},{"key":"12","doi-asserted-by":"crossref","unstructured":"L Xie, J Zhao, Y Li, et al.  \"Phys Life Rev.\"  49, \"PET brain imaging in neurological disorders.\" 100 (2024)","DOI":"10.1016\/j.plrev.2024.03.007"},{"key":"13","doi-asserted-by":"crossref","unstructured":"S Amadoru, V Dore, CA McLean, et al.  \"Alzheimers Res Ther.\"  12, \"Comparison of amyloid PET measured in Centiloid units with neuropathological findings in Alzheimer's disease.\" 22 (2020)","DOI":"10.1186\/s13195-020-00587-5"},{"key":"14","doi-asserted-by":"crossref","unstructured":"K Chen  and PS Conti  \"Adv Drug Deliv Rev.\"  62, \"Target-specific delivery of peptide-based probes for PET imaging.\" 1005 (2010)","DOI":"10.1016\/j.addr.2010.09.004"},{"key":"15","doi-asserted-by":"crossref","unstructured":"W Bao, F Xie, C Zuo, et al.  \"Front Aging Neurosci.\"  13, \"PET Neuroimaging of Alzheimer's disease: Radiotracers and their utility in clinical research.\" 624330 (2021)","DOI":"10.3389\/fnagi.2021.624330"},{"key":"16","doi-asserted-by":"crossref","unstructured":"VJ Lowe, CT Mester, ES Lundt, et al.  \"Alzheimers Dement.\"  20, \"Amyloid PET detects the deposition of brain Abeta earlier than CSF fluid biomarkers.\" 8097 (2024)","DOI":"10.1002\/alz.14317"},{"key":"17","doi-asserted-by":"crossref","unstructured":"MR Flanigan, SK Royse, DP Cenkner, et al.  \"Transl Psychiatry.\"  11, \"Imaging beta-amyloid (Abeta) burden in the brains of middle-aged individuals with alcohol-use disorders: a [(11)C]PIB PET study.\" 257 (2021)","DOI":"10.1038\/s41398-021-01374-y"},{"key":"18","doi-asserted-by":"crossref","unstructured":"SJ Teipel, AGM Temp, F Levin, et al.  \"Ann Clin Transl Neurol.\"  8, \"Association of PET-based stages of amyloid deposition with neuropathological markers of Abeta pathology.\" 29 (2021)","DOI":"10.1002\/acn3.51238"},{"key":"19","doi-asserted-by":"crossref","unstructured":"AJ Kure, H Savas, TA Hijaz, et al.  \"Semin Ultrasound CT MR.\"  42, \"Advancements in positron emission tomography\/magnetic resonance imaging and applications to diagnostic challenges in neuroradiology.\" 434 (2021)","DOI":"10.1053\/j.sult.2021.07.002"},{"key":"20","doi-asserted-by":"crossref","unstructured":"WE Klunk, Y Wang, GF Huang, et al.  \"Life Sci.\"  69, \"Uncharged thioflavin-T derivatives bind to amyloid-beta protein with high affinity and readily enter the brain.\" 1471 (2001)","DOI":"10.1016\/S0024-3205(01)01232-2"},{"key":"21","doi-asserted-by":"crossref","unstructured":"CC Rowe, U Ackerman, W Browne, et al.  \"Lancet Neurol.\"  7, \"Imaging of amyloid beta in Alzheimer's disease with 18F-BAY94-9172, a novel PET tracer: proof of mechanism.\" 129 (2008)","DOI":"10.1016\/S1474-4422(08)70001-2"},{"key":"22","doi-asserted-by":"crossref","unstructured":"N Nelissen, K Van Laere, L Thurfjell, et al.  \"J Nucl Med.\"  50, \"Phase 1 study of the Pittsburgh compound B derivative 18F-flutemetamol in healthy volunteers and patients with probable Alzheimer disease.\" 1251 (2009)","DOI":"10.2967\/jnumed.109.063305"},{"key":"23","doi-asserted-by":"crossref","unstructured":"XT Fang, J Eriksson, G Antoni, et al.  \"Neuropharmacology.\"  113, \"Brain mGluR5 in mice with amyloid beta pathology studied with in vivo [(11)C]ABP688 PET imaging and ex vivo immunoblotting.\" 293 (2017)","DOI":"10.1016\/j.neuropharm.2016.10.009"},{"key":"24","doi-asserted-by":"crossref","unstructured":"HG Pemberton, LE Collij, F Heeman, et al.  \"Eur J Nucl Med Mol Imaging.\"  49, \"Quantification of amyloid PET for future clinical use: a state-of-the-art review.\" 3508 (2022)","DOI":"10.1007\/s00259-022-05784-y"},{"key":"25","doi-asserted-by":"crossref","unstructured":"A Lockhart, JR Lamb, T Osredkar, et al.  \"Brain.\"  130, \"PIB is a non-specific imaging marker of amyloid-beta (Abeta) peptide-related cerebral amyloidosis.\" 2607 (2007)","DOI":"10.1093\/brain\/awm191"},{"key":"26","doi-asserted-by":"crossref","unstructured":"A Kadir, A Marutle, D Gonzalez, et al.  \"Brain.\"  134, \"Positron emission tomography imaging and clinical progression in relation to molecular pathology in the first Pittsburgh compound B positron emission tomography patient with Alzheimer's disease.\" 301 (2011)","DOI":"10.1093\/brain\/awq349"},{"key":"27","doi-asserted-by":"crossref","unstructured":"N Villain, G Chetelat, B Grassiot, et al.  \"Brain.\"  135, \"Regional dynamics of amyloid-beta deposition in healthy elderly, mild cognitive impairment and Alzheimer's disease: a voxelwise PiB-PET longitudinal study.\" 2126 (2012)","DOI":"10.1093\/brain\/aws125"},{"key":"28","doi-asserted-by":"crossref","unstructured":"A Mohebbi, I Kiani, S Mohammadzadeh, et al.  \"Abdom Radiol (NY).\"  50, \"Qualitative and quantitative differentiation efficiency of dual-tracer PET\/CT with 18F-fluorodeoxyglucose and (11) C-acetate for primary hepatocellular carcinoma: a systematic review and meta-analysis.\" 198 (2025)","DOI":"10.1007\/s00261-024-04302-y"},{"key":"29","doi-asserted-by":"crossref","unstructured":"NA. Lassen,  \"Eur J Nucl Med.\"  23, \"A reappraisal of the relative merits of SPET and PET in the quantitation of neuroreceptors: the advantage of a longer half-life!\" 1 (1996)","DOI":"10.1007\/BF01736982"},{"key":"30","doi-asserted-by":"crossref","unstructured":"M Koole, DM Lewis, C Buckley, et al.  \"J Nucl Med.\"  50, \"Whole-body biodistribution and radiation dosimetry of 18F-GE067: a radioligand for in vivo brain amyloid imaging.\" 818 (2009)","DOI":"10.2967\/jnumed.108.060756"},{"key":"31","doi-asserted-by":"crossref","unstructured":"NP Verhoeff, AA Wilson, S Takeshita, et al.  \"Am J Geriatr Psychiatry.\"  12, \"In-vivo imaging of Alzheimer disease beta-amyloid with [11C]SB-13 PET.\" 584 (2004)","DOI":"10.1176\/appi.ajgp.12.6.584"},{"key":"32","doi-asserted-by":"crossref","unstructured":"W Zhang, S Oya, MP Kung, et al.  \"Nucl Med Biol.\"  32, \"F-18 Polyethyleneglycol stilbenes as PET imaging agents targeting Abeta aggregates in the brain.\" 799 (2005)","DOI":"10.1016\/j.nucmedbio.2005.06.001"},{"key":"33","doi-asserted-by":"crossref","unstructured":"W Zhang, MP Kung, S Oya, et al.  \"Nucl Med Biol.\"  34, \"18F-labeled styrylpyridines as PET agents for amyloid plaque imaging.\" 89 (2007)","DOI":"10.1016\/j.nucmedbio.2006.10.003"},{"key":"34","doi-asserted-by":"crossref","unstructured":"CM Clark, MJ Pontecorvo, TG Beach, et al.  \"Lancet Neurol.\"  11, \"Cerebral PET with florbetapir compared with neuropathology at autopsy for detection of neuritic amyloid-beta plaques: a prospective cohort study.\" 669 (2012)","DOI":"10.1016\/S1474-4422(12)70142-4"},{"key":"35","unstructured":"EM Reiman, JB Langbaum, AS Fleisher, et al.  \"J Alzheimers Dis.\"  26, \"Alzheimer's Prevention Initiative: a plan to accelerate the evaluation of presymptomatic treatments.\" 321 (2011)"},{"key":"36","doi-asserted-by":"crossref","unstructured":"PS Insel, MC Donohue, R Sperling, et al.  \"Ann Clin Transl Neurol.\"  7, \"The A4 study: beta-amyloid and cognition in 4432 cognitively unimpaired adults.\" 776 (2020)","DOI":"10.1002\/acn3.51048"},{"key":"37","doi-asserted-by":"crossref","unstructured":"L Rejc, D Knez, G Molina-Aguirre, et al.  \"Biomed Pharmacother.\"  175, \"Probing Alzheimer's pathology: Exploring the next generation of FDDNP analogues for amyloid beta detection.\" 116616 (2024)","DOI":"10.1016\/j.biopha.2024.116616"},{"key":"38","doi-asserted-by":"crossref","unstructured":"B Krause-Sorio, P Siddarth, KT Laird, et al.  \"Int Psychogeriatr.\"  33, \"FDDNP PET binding predicts change in executive function in a pilot clinical trial of geriatric depression.\" 149 (18)","DOI":"10.1017\/S1041610219002047"},{"key":"39","doi-asserted-by":"crossref","unstructured":"C Curtis, JE Gamez, U Singh, et al.  \"JAMA Neurol.\"  72, \"Phase 3 trial of flutemetamol labeled with radioactive fluorine 18 imaging and neuritic plaque density.\" 287 (2015)","DOI":"10.1001\/jamaneurol.2014.4144"},{"key":"40","doi-asserted-by":"crossref","unstructured":"S Hatashita, H Yamasaki, Y Suzuki, et al.  \"Eur J Nucl Med Mol Imaging.\"  41, \"Flutemetamol amyloid-beta PET imaging compared with [11C]PIB across the spectrum of Alzheimer's disease.\" 290 (2014)","DOI":"10.1007\/s00259-013-2564-y"},{"key":"41","doi-asserted-by":"crossref","unstructured":"H Barthel, HJ Gertz, S Dresel, et al.  \"Lancet Neurol.\"  10, \"Cerebral amyloid-beta PET with florbetaben (18F) in patients with Alzheimer's disease and healthy controls: a multicentre phase 2 diagnostic study.\" 424 (2011)","DOI":"10.1016\/S1474-4422(11)70077-1"},{"key":"42","doi-asserted-by":"crossref","unstructured":"O Sabri, MN Sabbagh, J Seibyl, et al.  \"Alzheimers Dement.\"  11, \"Florbetaben PET imaging to detect amyloid beta plaques in Alzheimer's disease: phase 3 study.\" 964 (2015)","DOI":"10.1016\/j.jalz.2015.02.004"},{"key":"43","doi-asserted-by":"crossref","unstructured":"AE Kassab, EM Gedawy, AS Sayed,  \"Int J Biol Macromol.\"  265, \"Fused thiophene as a privileged scaffold: A review on anti-Alzheimer's disease potentials via targeting cholinesterases, monoamine oxidases, glycogen synthase kinase-3, and Abeta aggregation.\" 131018 (2024)","DOI":"10.1016\/j.ijbiomac.2024.131018"},{"key":"44","doi-asserted-by":"crossref","unstructured":"S Kaide, H Watanabe, Y Shimizu, et al.  \"ACS Chem Neurosci.\"  11, \"Identification and evaluation of bisquinoline scaffold as a new candidate for alpha-synuclein-PET imaging.\" 4254 (2020)","DOI":"10.1021\/acschemneuro.0c00523"},{"key":"45","doi-asserted-by":"crossref","unstructured":"A Singh, A Verma, B Bhardwaj, et al.  \"ACS Omega.\"  9, \"Structure-guided design, synthesis, and biological evaluation of peripheral anionic site selective and brain permeable novel oxadiazole-piperazine conjugates against Alzheimer's disease with antioxidant potential.\" 18169 (2024)","DOI":"10.1021\/acsomega.3c10276"},{"key":"46","doi-asserted-by":"crossref","unstructured":"A Horton, K Nash, E Tackie-Yarboi, et al.  \"J Med Chem.\"  61, \"Furoxans (Oxadiazole-4 N-oxides) with attenuated reactivity are neuroprotective, cross the blood brain barrier, and improve passive avoidance memory.\" 4593 (2018)","DOI":"10.1021\/acs.jmedchem.8b00389"},{"key":"47","doi-asserted-by":"crossref","unstructured":"M Saitoh, J Kunitomo, E Kimura, et al.  \"J Med Chem.\"  52, \"2-3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl-5-methy-l-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.\" 6270 (2009)","DOI":"10.1021\/jm900647e"},{"key":"48","doi-asserted-by":"crossref","unstructured":"H Fu, P Tu, L Zhao, et al.  \"Anal Chem.\"  88, \"Amyloid-beta deposits target efficient near-infrared fluorescent probes: Synthesis, in vitro evaluation, and in vivo imaging.\" 1944 (2016)","DOI":"10.1021\/acs.analchem.5b04441"},{"key":"49","doi-asserted-by":"crossref","unstructured":"K Zhou, H Fu, L Feng, et al.  \"Chem Commun (Camb).\"  51, \"The synthesis and evaluation of near-infrared probes with barbituric acid acceptors for in vivo detection of amyloid plaques.\" 11665 (2015)","DOI":"10.1039\/C5CC03662C"},{"key":"50","doi-asserted-by":"crossref","unstructured":"Y Li, K Zhou, X Zhang, et al.  \"J Med Chem.\"  66, \"Fluorine-18-labeled diaryl-azines as improved beta-amyloid imaging tracers: From bench to first-in-human studies.\" 4603 (2023)","DOI":"10.1021\/acs.jmedchem.2c01503"},{"key":"51","doi-asserted-by":"crossref","unstructured":"T Liu, Y Li, X Zhang, et al.  \"J Med Chem.\"  66, \"Synthesis and preclinical evaluation of 2-(4-[(18)F]Fluorophenyl)imidazo [1,2-h][1,7]naphthyridine ([(18)F]FPND-4): An aza-fused tricyclic derivative as positron emission tomography tracer for neurofibrillary tangle imaging.\" 9561 (2023)","DOI":"10.1021\/acs.jmedchem.3c00239"},{"key":"52","doi-asserted-by":"crossref","unstructured":"Y Li, K Zhou, W Guo, et al.  \"Bioorg Med Chem.\"  29, \"F-labeled 2-phenylbenzohe-terocycles with chiral dihydroxyl side chains as beta-amyloid imaging probes.\" 115884 (2021)","DOI":"10.1016\/j.bmc.2020.115884"},{"key":"53","doi-asserted-by":"crossref","unstructured":"H Fu, L Yu, M Cui, et al.  \"Bioorg Med Chem.\"  21, \"Synthesis and biological evaluation of 18F-labled 2-phenylindole derivatives as PET imaging probes for beta-amyloid plaques.\" 3708 (2013)","DOI":"10.1016\/j.bmc.2013.04.028"},{"key":"54","doi-asserted-by":"crossref","unstructured":"H Fu, M Cui, L Zhao, et al.  \"J Med Chem.\"  58, \"Highly sensitive near-infrared fluorophores for in vivo detection of amyloid-beta plaques in Alzheimer's disease.\" 6972 (2015)","DOI":"10.1021\/acs.jmedchem.5b00861"},{"key":"1","doi-asserted-by":"crossref","unstructured":"J Hardy  and DJ Selkoe  \"Science.\"  297, \"The amyloid hypothesis of Alzheimer's disease: progress and problems on the road to therapeutics.\" 353 (2002)","DOI":"10.1126\/science.1072994"}],"container-title":["Radiation Research"],"original-title":[],"link":[{"URL":"https:\/\/meridian.allenpress.com\/radiation-research\/article-pdf\/doi\/10.1667\/RADE-25-00035.1\/3502652\/10.1667_rade-25-00035.1.pdf","content-type":"application\/pdf","content-version":"vor","intended-application":"syndication"},{"URL":"https:\/\/meridian.allenpress.com\/radiation-research\/article-pdf\/doi\/10.1667\/RADE-25-00035.1\/3502652\/10.1667_rade-25-00035.1.pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2026,10,5]],"date-time":"2026-10-05T23:27:16Z","timestamp":1791242836000},"score":1,"resource":{"primary":{"URL":"https:\/\/bioone.org\/journals\/radiation-research\/volume-203\/issue-5\/RADE-25-00035.1\/Synthesis-and-Evaluation-of-Novel-18F-labeled-Oxadiazole-based-Positron\/10.1667\/RADE-25-00035.1.full"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2025,3,24]]},"references-count":54,"journal-issue":{"issue":"5","published-online":{"date-parts":[[2025,5,1]]}},"URL":"https:\/\/doi.org\/10.1667\/rade-25-00035.1","relation":{},"ISSN":["0033-7587","1938-5404"],"issn-type":[{"value":"0033-7587","type":"print"},{"value":"1938-5404","type":"electronic"}],"subject":[],"published":{"date-parts":[[2025,3,24]]}}}