Literature DB >> 26101580

Synthesis and evaluation of [11C]PBD150, a radiolabeled glutaminyl cyclase inhibitor for the potential detection of Alzheimer's disease prior to amyloid β aggregation.

Allen F Brooks1, Isaac M Jackson1, Xia Shao1, George W Kropog1, Phillip Sherman1, Carole A Quesada1, Peter J H Scott2.   

Abstract

The phenol of 1-(3-(1H-imidazol-1-yl)propyl)-3-(4-hydroxy-3-methoxyphenyl)thiourea was selectively carbon-11 labelled to generate [11C]PBD150 in 7.3% yield from [11C]methyl triflate (non-decay corrected; radiochemical purity ≥95%, specific activity = 5.7 Ci/µmol, n=5). Evaluation of [11C]PBD150 by small animal PET imaging (mouse and rat) determined it does not permeate the blood brain barrier, indicating previously described therapeutic effect in transgenic mice was likely not the result of inhibiting central nervous system glutaminyl cyclase.

Entities:  

Year:  2015        PMID： 26101580      PMCID： PMC4474278          DOI： 10.1039/C5MD00148J

Source DB:  PubMed          Journal:  Medchemcomm        ISSN： 2040-2503            Impact factor:   3.597


  20 in total

1.  Structure-activity relationships of benzimidazole-based glutaminyl cyclase inhibitors featuring a heteroaryl scaffold.

Authors:  Daniel Ramsbeck; Mirko Buchholz; Birgit Koch; Livia Böhme; Torsten Hoffmann; Hans-Ulrich Demuth; Ulrich Heiser
Journal:  J Med Chem       Date:  2013-08-19       Impact factor: 7.446

2.  Inhibitors for human glutaminyl cyclase by structure based design and bioisosteric replacement.

Authors:  Mirko Buchholz; Antje Hamann; Susanne Aust; Wolfgang Brandt; Livia Böhme; Torsten Hoffmann; Stephan Schilling; Hans-Ulrich Demuth; Ulrich Heiser
Journal:  J Med Chem       Date:  2009-11-26       Impact factor: 7.446

3.  The first potent inhibitors for human glutaminyl cyclase: synthesis and structure-activity relationship.

Authors:  Mirko Buchholz; Ulrich Heiser; Stephan Schilling; André J Niestroj; Katrin Zunkel; Hans-Ulrich Demuth
Journal:  J Med Chem       Date:  2006-01-26       Impact factor: 7.446

4.  Synthesis of guanidinium-derived receptor libraries and screening for selective peptide receptors in water.

Authors:  Kim B Jensen; Tobias M Braxmeier; Mariangela Demarcus; Jeremy G Frey; Jeremy D Kilburn
Journal:  Chemistry       Date:  2002-03-15       Impact factor: 5.236

5.  Chaperone activity of bicyclic nojirimycin analogues for Gaucher mutations in comparison with N-(n-nonyl)deoxynojirimycin.

Authors:  Zhuo Luan; Katsumi Higaki; Matilde Aguilar-Moncayo; Haruaki Ninomiya; Kousaku Ohno; M Isabel García-Moreno; Carmen Ortiz Mellet; José M García Fernández; Yoshiyuki Suzuki
Journal:  Chembiochem       Date:  2009-11-23       Impact factor: 3.164

6.  Enhanced radiosyntheses of [¹¹C]raclopride and [¹¹C]DASB using ethanolic loop chemistry.

Authors:  Xia Shao; Paul L Schnau; Maria V Fawaz; Peter J H Scott
Journal:  Nucl Med Biol       Date:  2012-11-02       Impact factor: 2.408

7.  Glutaminyl cyclase inhibition attenuates pyroglutamate Abeta and Alzheimer's disease-like pathology.

Authors:  Stephan Schilling; Ulrike Zeitschel; Torsten Hoffmann; Ulrich Heiser; Mike Francke; Astrid Kehlen; Max Holzer; Birgit Hutter-Paier; Manuela Prokesch; Manfred Windisch; Wolfgang Jagla; Dagmar Schlenzig; Christiane Lindner; Thomas Rudolph; Gunter Reuter; Holger Cynis; Dirk Montag; Hans-Ulrich Demuth; Steffen Rossner
Journal:  Nat Med       Date:  2008-09-28       Impact factor: 53.440

8.  Glutaminyl cyclase in human cortex: correlation with (pGlu)-amyloid-β load and cognitive decline in Alzheimer's disease.

Authors:  Markus Morawski; Stephan Schilling; Moritz Kreuzberger; Alexander Waniek; Carsten Jäger; Birgit Koch; Holger Cynis; Astrid Kehlen; Thomas Arendt; Maike Hartlage-Rübsamen; Hans-Ulrich Demuth; Steffen Roßner
Journal:  J Alzheimers Dis       Date:  2014       Impact factor: 4.472

9.  Structure-activity relationship of human glutaminyl cyclase inhibitors having an N-(5-methyl-1H-imidazol-1-yl)propyl thiourea template.

Authors:  Phuong-Thao Tran; Van-Hai Hoang; Shivaji A Thorat; Sung Eun Kim; Jihyae Ann; Yu Jin Chang; Dong Woo Nam; Hyundong Song; Inhee Mook-Jung; Jiyoun Lee; Jeewoo Lee
Journal:  Bioorg Med Chem       Date:  2013-04-17       Impact factor: 3.641

10.  Prion-like behaviour and tau-dependent cytotoxicity of pyroglutamylated amyloid-β.

Authors:  Justin M Nussbaum; Stephan Schilling; Holger Cynis; Antonia Silva; Eric Swanson; Tanaporn Wangsanut; Kaycie Tayler; Brian Wiltgen; Asa Hatami; Raik Rönicke; Klaus Reymann; Birgit Hutter-Paier; Anca Alexandru; Wolfgang Jagla; Sigrid Graubner; Charles G Glabe; Hans-Ulrich Demuth; George S Bloom
Journal:  Nature       Date:  2012-05-02       Impact factor: 49.962
View more
  5 in total

1.  In vitro and in silico determination of glutaminyl cyclase inhibitors.

Authors:  Phuong-Thao Tran; Van-Hai Hoang; Jeewoo Lee; Tran Thi Thu Hien; Nguyen Thanh Tung; Son Tung Ngo
Journal:  RSC Adv       Date:  2019-09-19       Impact factor: 4.036

2.  Synthesis and Evaluation of [(18)F]RAGER: A First Generation Small-Molecule PET Radioligand Targeting the Receptor for Advanced Glycation Endproducts.

Authors:  Brian P Cary; Allen F Brooks; Maria V Fawaz; Lindsey R Drake; Timothy J Desmond; Phillip Sherman; Carole A Quesada; Peter J H Scott
Journal:  ACS Chem Neurosci       Date:  2016-02-01       Impact factor: 4.418

3.  Synthesis of Diverse (11)C-Labeled PET Radiotracers via Direct Incorporation of [(11)C]CO2.

Authors:  Andrew V Mossine; Allen F Brooks; Isaac M Jackson; Carole A Quesada; Phillip Sherman; Erin L Cole; David J Donnelly; Peter J H Scott; Xia Shao
Journal:  Bioconjug Chem       Date:  2016-04-14       Impact factor: 4.774

Review 4.  Symptomatic and Disease-Modifying Therapy Pipeline for Alzheimer's Disease: Towards a Personalized Polypharmacology Patient-Centered Approach.

Authors:  Xavier Morató; Vanesa Pytel; Sara Jofresa; Agustín Ruiz; Mercè Boada
Journal:  Int J Mol Sci       Date:  2022-08-18       Impact factor: 6.208

5.  Sulfur-containing therapeutics in the treatment of Alzheimer's disease.

Authors:  Haizhou Zhu; Venkateshwara Dronamraju; Wei Xie; Swati S More
Journal:  Med Chem Res       Date:  2021-01-15       Impact factor: 1.965
  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.