Literature DB >> 17850126

New series of antiprion compounds: pyrazolone derivatives have the potent activity of inhibiting protease-resistant prion protein accumulation.

Ayako Kimata1, Hidehiko Nakagawa, Ryo Ohyama, Tomoko Fukuuchi, Shigeru Ohta, Katsumi Doh-ura, Takayoshi Suzuki, Naoki Miyata.   

Abstract

To find effective antiprion compounds, we synthesized and evaluated various pyrazolone derivatives. Seven of 19 compounds showed inhibition of PrP-res accumulation and the remarkably active compound 13 showed an IC50 value of 3 nM in both ScN2a and F3 cell lines. Findings from studies on physicochemical and biochemical properties suggest that the action mechanism of these compounds does not correlate with any antioxidant activities, any of hydroxyl radical scavenging activities, or any SOD-like activities.

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Year:  2007        PMID: 17850126     DOI: 10.1021/jm070688r

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  21 in total

1.  Pharmacokinetics and metabolism of 2-aminothiazoles with antiprion activity in mice.

Authors:  B Michael Silber; Satish Rao; Kimberly L Fife; Alejandra Gallardo-Godoy; Adam R Renslo; Deepak K Dalvie; Kurt Giles; Yevgeniy Freyman; Manuel Elepano; Joel R Gever; Zhe Li; Matthew P Jacobson; Yong Huang; Leslie Z Benet; Stanley B Prusiner
Journal:  Pharm Res       Date:  2013-02-16       Impact factor: 4.200

2.  A Promising Antiprion Trimethoxychalcone Binds to the Globular Domain of the Cellular Prion Protein and Changes Its Cellular Location.

Authors:  N C Ferreira; L M Ascari; A G Hughson; G R Cavalheiro; C F Góes; P N Fernandes; J R Hollister; R A da Conceição; D S Silva; A M T Souza; M L C Barbosa; F A Lara; R A P Martins; B Caughey; Y Cordeiro
Journal:  Antimicrob Agents Chemother       Date:  2018-01-25       Impact factor: 5.191

3.  Cellular prion protein (PrPC) in the development of Merlin-deficient tumours.

Authors:  L Provenzano; Y Ryan; D A Hilton; J Lyons-Rimmer; F Dave; E A Maze; C L Adams; R Rigby-Jones; S Ammoun; C O Hanemann
Journal:  Oncogene       Date:  2017-07-10       Impact factor: 9.867

4.  Quinacrine promotes replication and conformational mutation of chronic wasting disease prions.

Authors:  Jifeng Bian; Hae-Eun Kang; Glenn C Telling
Journal:  Proc Natl Acad Sci U S A       Date:  2014-04-07       Impact factor: 11.205

5.  Metal-free arylation of ethyl acetoacetate with hypervalent diaryliodonium salts: an immediate access to diverse 3-aryl-4(1H)-quinolones.

Authors:  Andrii Monastyrskyi; Niranjan K Namelikonda; Roman Manetsch
Journal:  J Org Chem       Date:  2015-02-24       Impact factor: 4.354

6.  2-Aminothiazoles as therapeutic leads for prion diseases.

Authors:  Alejandra Gallardo-Godoy; Joel Gever; Kimberly L Fife; B Michael Silber; Stanley B Prusiner; Adam R Renslo
Journal:  J Med Chem       Date:  2011-01-19       Impact factor: 7.446

Review 7.  Recent advances in prion chemotherapeutics.

Authors:  Valerie L Sim; Byron Caughey
Journal:  Infect Disord Drug Targets       Date:  2009-02

8.  2-Aminothiazoles with improved pharmacotherapeutic properties for treatment of prion disease.

Authors:  Zhe Li; B Michael Silber; Satish Rao; Joel R Gever; Clifford Bryant; Alejandra Gallardo-Godoy; Elena Dolghih; Kartika Widjaja; Manuel Elepano; Matthew P Jacobson; Stanley B Prusiner; Adam R Renslo
Journal:  ChemMedChem       Date:  2013-03-18       Impact factor: 3.466

9.  Characterizing antiprion compounds based on their binding properties to prion proteins: implications as medical chaperones.

Authors:  Yuji O Kamatari; Yosuke Hayano; Kei-ichi Yamaguchi; Junji Hosokawa-Muto; Kazuo Kuwata
Journal:  Protein Sci       Date:  2012-11-19       Impact factor: 6.725

10.  Unique drug screening approach for prion diseases identifies tacrolimus and astemizole as antiprion agents.

Authors:  Yervand Eduard Karapetyan; Gian Franco Sferrazza; Minghai Zhou; Gregory Ottenberg; Timothy Spicer; Peter Chase; Mohammad Fallahi; Peter Hodder; Charles Weissmann; Corinne Ida Lasmézas
Journal:  Proc Natl Acad Sci U S A       Date:  2013-04-01       Impact factor: 11.205

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