Literature DB >> 23585921

Synthesis and in vitro biological evaluation of pyrazole group-containing analogues for PDE10A.

Junfeng Li1, Hongjun Jin, Haiying Zhou, Justin Rothfuss, Zhude Tu.   

Abstract

Twenty eight new analogues were synthesized by optimizing the structure of MP-10 and their in vitro binding affinities towards PDE10A, PDE3A/B, and PDE4A/B were determined. Among these new analogues, 10a, 10b, 10d, 11a, 11b and 11d are very potent towards PDE10A and have IC50 values of 0.40 ± 0.02, 0.28 ± 0.06, 1.82 ± 0.25, 0.24 ± 0.05, 0.36 ± 0.03 and 1.78 ± 0.03 nM respectively; these six compounds displayed high selectivity for PDE10A versus PDE3A/3B/4A/4B. The promising compounds will be further validated in vivo to identify PDE10A imaging tracers.

Entities:  

Year:  2013        PMID： 23585921      PMCID： PMC3625062          DOI： 10.1039/C2MD20239E

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


  25 in total

1.  Cloning and characterization of a novel human phosphodiesterase that hydrolyzes both cAMP and cGMP (PDE10A).

Authors:  K Fujishige; J Kotera; H Michibata; K Yuasa; S Takebayashi; K Okumura; K Omori
Journal:  J Biol Chem       Date:  1999-06-25       Impact factor: 5.157

Review 2.  Patented PDE10A inhibitors: novel compounds since 2007.

Authors:  Jan Kehler; John Paul Kilburn
Journal:  Expert Opin Ther Pat       Date:  2009-12       Impact factor: 6.674

3.  Radiosynthesis and in vivo evaluation of [11C]MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brain.

Authors:  Zhude Tu; Jinda Fan; Shihong Li; Lynne A Jones; Jinquan Cui; Prashanth K Padakanti; Jinbin Xu; Dexing Zeng; Kooresh I Shoghi; Joel S Perlmutter; Robert H Mach
Journal:  Bioorg Med Chem       Date:  2011-01-22       Impact factor: 3.641

4.  Isolation and characterization of PDE10A, a novel human 3', 5'-cyclic nucleotide phosphodiesterase.

Authors:  K Loughney; P B Snyder; L Uher; G J Rosman; K Ferguson; V A Florio
Journal:  Gene       Date:  1999-06-24       Impact factor: 3.688

5.  Isolation and characterization of a dual-substrate phosphodiesterase gene family: PDE10A.

Authors:  S H Soderling; S J Bayuga; J A Beavo
Journal:  Proc Natl Acad Sci U S A       Date:  1999-06-08       Impact factor: 11.205

6.  Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia.

Authors:  Patrick R Verhoest; Douglas S Chapin; Michael Corman; Kari Fonseca; John F Harms; Xinjun Hou; Eric S Marr; Frank S Menniti; Frederick Nelson; Rebecca O'Connor; Jayvardhan Pandit; Caroline Proulx-Lafrance; Anne W Schmidt; Christopher J Schmidt; Judith A Suiciak; Spiros Liras
Journal:  J Med Chem       Date:  2009-08-27       Impact factor: 7.446

7.  Striatal phosphodiesterase mRNA and protein levels are reduced in Huntington's disease transgenic mice prior to the onset of motor symptoms.

Authors:  A L O Hebb; H A Robertson; E M Denovan-Wright
Journal:  Neuroscience       Date:  2004       Impact factor: 3.590

8.  Development of a cell-based assay for screening of phosphodiesterase 10A (PDE10A) inhibitors using a stable recombinant HEK-293 cell line expressing high levels of PDE10A.

Authors:  Roop Singh Bora; Dikshi Gupta; Renu Malik; Sonia Chachra; Pratibha Sharma; Kulvinder Singh Saini
Journal:  Biotechnol Appl Biochem       Date:  2008-02       Impact factor: 2.431

9.  Emetic, central nervous system, and pulmonary activities of rolipram in the dog.

Authors:  R J Heaslip; D Y Evans
Journal:  Eur J Pharmacol       Date:  1995-11-24       Impact factor: 4.432

Review 10.  Recent advances in positron emission tomography (PET) radiotracers for imaging phosphodiesterases.

Authors:  José Ignacio Andrés; Meri De Angelis; Jesús Alcázar; Sofie Celen; Guy Bormans
Journal:  Curr Top Med Chem       Date:  2012       Impact factor: 3.295
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  9 in total

1.  In Vivo Characterization of Two 18F-Labeled PDE10A PET Radioligands in Nonhuman Primate Brains.

Authors:  Hui Liu; Hongjun Jin; Zonghua Luo; Xuyi Yue; Xiang Zhang; Hubert Flores; Yi Su; Joel S Perlmutter; Zhude Tu
Journal:  ACS Chem Neurosci       Date:  2018-02-19       Impact factor: 4.418

2.  Application of 2,4-bis(halomethyl)quinoline: synthesis and biological activities of 2,4-bis(benzofuran-2-yl)- and 2,4-bis(aroxymethyl)quinolines.

Authors:  Yang Li; Qiqi Xu; Zhiyuan Li; Wentao Gao; Yu Chen
Journal:  Mol Divers       Date:  2019-03-20       Impact factor: 2.943

3.  Synthesis of Fluorine-Containing Phosphodiesterase 10A (PDE10A) Inhibitors and the In Vivo Evaluation of F-18 Labeled PDE10A PET Tracers in Rodent and Nonhuman Primate.

Authors:  Junfeng Li; Xiang Zhang; Hongjun Jin; Jinda Fan; Hubert Flores; Joel S Perlmutter; Zhude Tu
Journal:  J Med Chem       Date:  2015-10-15       Impact factor: 7.446

4.  Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.

Authors:  Hao Yang; Francis N Murigi; Zhijian Wang; Junfeng Li; Hongjun Jin; Zhude Tu
Journal:  Bioorg Med Chem Lett       Date:  2014-12-22       Impact factor: 2.823

5.  Preclinical evaluation of a promising C-11 labeled PET tracer for imaging phosphodiesterase 10A in the brain of living subject.

Authors:  Hui Liu; Hongjun Jin; Xuyi Yue; Xiang Zhang; Hao Yang; Junfeng Li; Hubert Flores; Yi Su; Joel S Perlmutter; Zhude Tu
Journal:  Neuroimage       Date:  2015-07-26       Impact factor: 6.556

6.  Radiosyntheses and in vivo evaluation of carbon-11 PET tracers for PDE10A in the brain of rodent and nonhuman primate.

Authors:  Jinda Fan; Xiang Zhang; Junfeng Li; Hongjun Jin; Prashanth K Padakanti; Lynne A Jones; Hubert P Flores; Yi Su; Joel S Perlmutter; Zhude Tu
Journal:  Bioorg Med Chem       Date:  2014-03-26       Impact factor: 3.641

Review 7.  Pyrazole Scaffold Synthesis, Functionalization, and Applications in Alzheimer's Disease and Parkinson's Disease Treatment (2011-2020).

Authors:  Xuefei Li; Yanbo Yu; Zhude Tu
Journal:  Molecules       Date:  2021-02-24       Impact factor: 4.411

Review 8.  Challenges on Cyclic Nucleotide Phosphodiesterases Imaging with Positron Emission Tomography: Novel Radioligands and (Pre-)Clinical Insights since 2016.

Authors:  Susann Schröder; Matthias Scheunemann; Barbara Wenzel; Peter Brust
Journal:  Int J Mol Sci       Date:  2021-04-07       Impact factor: 5.923

9.  Comparison of [11C]TZ1964B and [18F]MNI659 for PET imaging brain PDE10A in nonhuman primates.

Authors:  Hui Liu; Hongjun Jin; Xuyi Yue; Junbin Han; Hao Yang; Hubert Flores; Yi Su; David Alagille; Joel S Perlmutter; Gilles Tamagnan; Zhude Tu
Journal:  Pharmacol Res Perspect       Date:  2016-08-26
  9 in total

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