Tideglusib

Tideglusib
Identifiers


IUPAC name 4-Benzyl-2-(naphthalen-1-yl)-1,2,4-thiadiazolidine-3,5-dione
PubChem (CID)	11313622
ChemSpider	9488589
Chemical and physical data
Formula	C₁₉H₁₄N₂O₂S
Molar mass	334.392 g/mol
3D model (Jmol)	Interactive image
SMILES O=C3SN(c1cccc2c1cccc2)C(=O)N3Cc4ccccc4
InChI InChI=1S/C19H14N2O2S/c22-18-20(13-14-7-2-1-3-8-14)19(23)24-21(18)17-12-6-10-15-9-4-5-11-16(15)17/h1-12H,13H2

Tideglusib (NP-12, NP031112) is a potent, selective and irreversible^[1] small molecule non-ATP-competitive GSK3 inhibitor that has been investigated as a potential treatment for Alzheimer's disease and paralysis supranuclear palsy in Phase IIa^[2] and IIb clinical trials.^[3]^[4]^[5]^[6] The first clinical trial conducted with tideglusib to be published (in English, at least) was phase II and demonstrated that overall tideglusib was well tolerated, except for some moderate, asymptomatic, fully reversible increases in liver enzymes (≥2.5xULN; where ULN=Upper Limit of Normal).^[4]

Reference List

↑ Domínguez, JM; Fuertes, A; Orozco, L; del Monte-Millán, M; Delgado, E; Medina, M (January 2012). "Evidence for Irreversible Inhibition of Glycogen Synthase Kinase-3 by Tideglusib" (PDF). The Journal of Biological Chemistry. 287 (2): 893–904. doi:10.1074/jbc.M111.306472. PMC 3256883. PMID 22102280.
↑ Teodoro Del Ser (2010). "Phase IIa clinical trial on Alzheimer's disease with NP12, a GSK3 inhibitor". Alzheimer's & Dementia. 6 (4): S147. doi:10.1016/j.jalz.2010.05.455.
↑ Eldar-Finkelman, H; Martinez, A (2011). "GSK-3 Inhibitors: Preclinical and Clinical Focus on CNS". Frontiers in Molecular Neuroscience. 4: 32. doi:10.3389/fnmol.2011.00032. PMC 3204427. PMID 22065134.
1 2 Del Ser, T; Steinwachs, KC; Gertz, HJ; Andrés, MV; Gómez-Carrillo, B; Medina, M; Vericat, JA; Redondo, P; et al. (2013). "Treatment of Alzheimer's disease with the GSK-3 inhibitor tideglusib: A pilot study". Journal of Alzheimer's disease. 33 (1): 205–15. doi:10.3233/JAD-2012-120805. PMID 22936007.
↑ "FDA Grants Fast Track Status to Tideglusib (ZentylorTM) for Progressive Supranuclear Palsy". PR Newswire Europe Including UK Disclose. 10 September 2010. Retrieved 11 August 2013.
↑ Dominguez, JM; Fuertes, A; Orozco, L; Del Monte-Millan, M; Delgado, E; Medina, M (2011). "Evidence for Irreversible Inhibition of Glycogen Synthase Kinase-3 by Tideglusib". Journal of Biological Chemistry. 287 (2): 893–904. doi:10.1074/jbc.M111.306472. PMC 3256883. PMID 22102280.

This article is issued from Wikipedia - version of the 8/5/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.