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

Li Z, Silber BM, Rao S, Gever JR, Bryant C, Gallardo-Godoy A, Dolghih E, Widjaja K, Elepano M, Jacobson MP, Prusiner SB, Renslo AR.

ChemMedChem. 2013 May;8(5):847-57. doi: 10.1002/cmdc.201300007. Epub 2013 Mar 18.


2-Aminothiazoles as therapeutic leads for prion diseases.

Gallardo-Godoy A, Gever J, Fife KL, Silber BM, Prusiner SB, Renslo AR.

J Med Chem. 2011 Feb 24;54(4):1010-21. doi: 10.1021/jm101250y. Epub 2011 Jan 19.


Discovery of 2-aminothiazoles as potent antiprion compounds.

Ghaemmaghami S, May BC, Renslo AR, Prusiner SB.

J Virol. 2010 Apr;84(7):3408-12. doi: 10.1128/JVI.02145-09. Epub 2009 Dec 23.


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

Silber BM, Rao S, Fife KL, Gallardo-Godoy A, Renslo AR, Dalvie DK, Giles K, Freyman Y, Elepano M, Gever JR, Li Z, Jacobson MP, Huang Y, Benet LZ, Prusiner SB.

Pharm Res. 2013 Apr;30(4):932-50. doi: 10.1007/s11095-012-0912-4. Epub 2013 Feb 16.


Aminothiazoles: Hit to lead development to identify antileishmanial agents.

Bhuniya D, Mukkavilli R, Shivahare R, Launay D, Dere RT, Deshpande A, Verma A, Vishwakarma P, Moger M, Pradhan A, Pati H, Gopinath VS, Gupta S, Puri SK, Martin D.

Eur J Med Chem. 2015 Sep 18;102:582-93. doi: 10.1016/j.ejmech.2015.08.013. Epub 2015 Aug 11.


In silico studies and fluorescence binding assays of potential anti-prion compounds reveal an important binding site for prion inhibition from PrP(C) to PrP(Sc).

Pagadala NS, Perez-Pineiro R, Wishart DS, Tuszynski JA.

Eur J Med Chem. 2015 Feb 16;91:118-31. doi: 10.1016/j.ejmech.2014.07.045. Epub 2014 Jul 15.


Successes and challenges in phenotype-based lead discovery for prion diseases.

Ghaemmaghami S, Russo M, Renslo AR.

J Med Chem. 2014 Aug 28;57(16):6919-29. doi: 10.1021/jm5001425. Epub 2014 Apr 24. Review.


Antiprion compounds that reduce PrP(Sc) levels in dividing and stationary-phase cells.

Silber BM, Gever JR, Li Z, Gallardo-Godoy A, Renslo AR, Widjaja K, Irwin JJ, Rao S, Jacobson MP, Ghaemmaghami S, Prusiner SB.

Bioorg Med Chem. 2013 Dec 15;21(24):7999-8012. doi: 10.1016/j.bmc.2013.09.022. Epub 2013 Sep 18.


Potent inhibition of scrapie prion replication in cultured cells by bis-acridines.

May BC, Fafarman AT, Hong SB, Rogers M, Deady LW, Prusiner SB, Cohen FE.

Proc Natl Acad Sci U S A. 2003 Mar 18;100(6):3416-21. Epub 2003 Mar 7.


Biaryl amides and hydrazones as therapeutics for prion disease in transgenic mice.

Lu D, Giles K, Li Z, Rao S, Dolghih E, Gever JR, Geva M, Elepano ML, Oehler A, Bryant C, Renslo AR, Jacobson MP, Dearmond SJ, Silber BM, Prusiner SB.

J Pharmacol Exp Ther. 2013 Nov;347(2):325-38. doi: 10.1124/jpet.113.205799. Epub 2013 Aug 21.


Improved 2,4-diarylthiazole-based antiprion agents: switching the sense of the amide group at C5 leads to an increase in potency.

Thompson MJ, Louth JC, Greenwood GK, Sorrell FJ, Knight SG, Adams NB, Chen B.

ChemMedChem. 2010 Sep 3;5(9):1476-88. doi: 10.1002/cmdc.201000217.


Continuous quinacrine treatment results in the formation of drug-resistant prions.

Ghaemmaghami S, Ahn M, Lessard P, Giles K, Legname G, DeArmond SJ, Prusiner SB.

PLoS Pathog. 2009 Nov;5(11):e1000673. doi: 10.1371/journal.ppat.1000673. Epub 2009 Nov 26.


Discovery of N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl}acetamide (TASP0415914) as an orally potent phosphoinositide 3-kinase γ inhibitor for the treatment of inflammatory diseases.

Oka Y, Yabuuchi T, Oi T, Kuroda S, Fujii Y, Ohtake H, Inoue T, Wakahara S, Kimura K, Fujita K, Endo M, Taguchi K, Sekiguchi Y.

Bioorg Med Chem. 2013 Dec 15;21(24):7578-83. doi: 10.1016/j.bmc.2013.10.042. Epub 2013 Nov 7.


Structure-activity relationships of 2-aminothiazoles effective against Mycobacterium tuberculosis.

Meissner A, Boshoff HI, Vasan M, Duckworth BP, Barry CE 3rd, Aldrich CC.

Bioorg Med Chem. 2013 Nov 1;21(21):6385-97. doi: 10.1016/j.bmc.2013.08.048. Epub 2013 Sep 3.


Antiprion activity of functionalized 9-aminoacridines related to quinacrine.

Nguyen TH, Lee CY, Teruya K, Ong WY, Doh-ura K, Go ML.

Bioorg Med Chem. 2008 Jul 15;16(14):6737-46. doi: 10.1016/j.bmc.2008.05.060. Epub 2008 Jun 13.


4-Bromo-2-(piperidin-1-yl)thiazol-5-yl-phenyl methanone (12b) inhibits Na+/K(+)-ATPase and Ras oncogene activity in cancer cells.

Lefranc F, Xu Z, Burth P, Mathieu V, Revelant G, de Castro Faria MV, Noyon C, Garcia DG, Dufour D, Bruyère C, Gonçalves-de-Albuquerque CF, Van Antwerpen P, Rogister B, Hesse S, Kirsch G, Kiss R.

Eur J Med Chem. 2013 May;63:213-23. doi: 10.1016/j.ejmech.2013.01.046. Epub 2013 Feb 16.


Discovery of novel 2-[2-(3-hydroxy-pyridin-2-yl)-thiazol-4-yl]-acetamide derivatives as HIF prolyl 4-hydroxylase inhibitors; SAR, synthesis and modeling evaluation.

Hong YR, Kim HT, Ro S, Cho JM, Lee SH, Kim IS, Jung YH.

Bioorg Med Chem Lett. 2014 Jul 15;24(14):3142-5. doi: 10.1016/j.bmcl.2014.05.003. Epub 2014 May 15.


Optimization of Arylamides as Novel, Potent and Brain-penetrant Antiprion Lead Compounds.

Li Z, Rao S, Gever JR, Widjaja K, Prusiner SB, Silber BM.

ACS Med Chem Lett. 2013 Jul 11;4(7):647-650.


Structure-based drug design identifies polythiophenes as antiprion compounds.

Herrmann US, Schütz AK, Shirani H, Huang D, Saban D, Nuvolone M, Li B, Ballmer B, Åslund AK, Mason JJ, Rushing E, Budka H, Nyström S, Hammarström P, Böckmann A, Caflisch A, Meier BH, Nilsson KP, Hornemann S, Aguzzi A.

Sci Transl Med. 2015 Aug 5;7(299):299ra123. doi: 10.1126/scitranslmed.aab1923.

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