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Tideglusib

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Also known as: 865854-05-3, Np031112, Np-12, 4-benzyl-2-(naphthalen-1-yl)-1,2,4-thiadiazolidine-3,5-dione, Tideglusib [inn], Np-031112

Molecular Formula

C₁₉H₁₄N₂O₂S

Molecular Weight

334.4 g/mol

InChI Key

PMJIHLSCWIDGMD-UHFFFAOYSA-N

FDA UNII

Q747Y6TT42

Tideglusib is under the investigation for the development of treatments for Alzheimer's disease and for progressive supranuclear palsy. It is reported to be a potent anti-inflammatory and neuroprotective that is a non-ATP competitive inhibitor of glycogen synthase kinase 3 (GSK-3). Tideglusib is being developed by the Spanish pharmaceutic company Zeltia group and its current status is withdrawn for the treatment of Alzheimer's disease as of 2012.

1 2D Structure

Tideglusib

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

4-benzyl-2-naphthalen-1-yl-1,2,4-thiadiazolidine-3,5-dione

2.1.2 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

2.1.3 InChI Key

PMJIHLSCWIDGMD-UHFFFAOYSA-N

2.1.4 Canonical SMILES

C1=CC=C(C=C1)CN2C(=O)N(SC2=O)C3=CC=CC4=CC=CC=C43

2.2 Other Identifiers

2.2.1 UNII

Q747Y6TT42

2.3 Synonyms

2.3.1 MeSH Synonyms

1. 4-benzyl-2-(naphthalene-1-yl)-1,2,4-thiadiazolidine-3,5-dione

2. Np 031112

3. Np-031112

4. Np-12 Compound

5. Np031112

6. Np12 Compound

2.3.2 Depositor-Supplied Synonyms

1. 865854-05-3

2. Np031112

3. Np-12

4. 4-benzyl-2-(naphthalen-1-yl)-1,2,4-thiadiazolidine-3,5-dione

5. Tideglusib [inn]

6. Np-031112

7. Np 031112

8. 4-benzyl-2-naphthalen-1-yl-1,2,4-thiadiazolidine-3,5-dione

9. Q747y6tt42

10. 1,2,4-thiadiazolidine-3,5-dione, 2-(1-naphthalenyl)-4-(phenylmethyl)-

11. 2-(1-naphthalenyl)-4-(phenylmethyl)-1,2,4-thiadiazolidine-3,5-dione

12. Tideglusibum

13. Zentylor

14. Nypta

15. Unii-q747y6tt42

16. Tideglusib [who-dd]

17. Tideglusib(np-031112)

18. Schembl676929

19. Gtpl6929

20. Chembl3545157

21. Tideglusib, >=98% (hplc)

22. Dtxsid90235682

23. Ex-a600

24. Chebi:147398

25. Hms3673g17

26. Hms3744e05

27. Hms3884j18

28. 4-benzyl-2-(naphthalen-1-yl)-(1,2,4)thiadiazolidine-3,5-dione

29. Bcp06016

30. Tideglusib,cas:865854-05-3

31. Bdbm50166940

32. Mfcd18633296

33. Nsc800950

34. S2823

35. Zinc13985228

36. Akos025149085

37. Ccg-267855

38. Cs-0613

39. Db12129

40. Nsc-800950

41. Sb19268

42. Tideglusib (np031112, Np-12)

43. Ncgc00386380-06

44. Ac-31056

45. As-56156

46. Da-41071

47. Hy-14872

48. Ft-0700382

49. A857027

50. J-514478

51. Q10382411

52. 4-benzyl-2-(a-naphtyl)-1,2,4-thiadiazolidine-3,5-dione

53. 4-benzyl-2-(a-naphthyl)-1,2,4-thiadiazolidine-3,5-dione

2.4 Create Date

2006-10-26

3 Chemical and Physical Properties

Molecular Formula	C₁₉H₁₄N₂O₂S
Molecular Weight	334.4 g/mol
XLogP3	4.3
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	3
Exact Mass	334.07759887 g/mol
Monoisotopic Mass	334.07759887 g/mol
Topological Polar Surface Area	65.9 Å²
Heavy Atom Count	24
Formal Charge	0
Complexity	492
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Indication

Tideglusib was initially formulated for the treatment of Alzheimer and progressive supranuclear palsy. The raising interest for the use of tideglusib comes from the significant upregulation of GSK-3 in the brain in patients with Alzheimer disease. Its function as a degradant of -catenin, was also important, as it prevents the transcription of cell survival genes. All these factors have directed current research towards this kinase as a potential target. Alzheimer disease is the most prevalent form of dementia. The most accepted hypothesis to explain this disease is related to the presence of amyloid , which triggers a cascade that will alter the Tau protein and provoke synaptic dysfunction and neuronal death. GSK-3 importance in the tissue repair pathway has also pointed out a novel application for tideglusib. Thus, it is also under the research for the natural repair treatment of deep caries lesions.

5 Pharmacology and Biochemistry

5.1 Pharmacology

It is reported that tideglusib administration inhibits the activation of astrocytes and microglial cells, thus it presented a neuroprotective effect. It is known as well that the inactivation of GSK-3 protects against excitotoxicity. In pre-clinical trials, there have been reports of decrease Tau hyperphosphorylation, lower brain amyloid plaque load, learning and memory enhancement, prevention of neuronal loss and significant increases of the insulin growth factor 1 which is a potent neurotrophic peptide with therapeutic value.The reports in clinical trials have shown a trend in cognition increase of Alzheimer patients treated for 24 weeks.

5.2 Mechanism of Action

GSK-3 is a proline/serine protein kinase that is ubiquitously expressed and involved in many cellular signaling pathways. From all its diverse functions, it plays a key role in Alzheimer's disease. This role is related to its link with -amyloid and tau pathology. It has been suggested that aberrant Wnt or insulin signaling results in increased GSK-3 function. This kinase acts on -secretase producing the hyperphosphorylation of tau, the formation of neurofibrillary tangles and senile plaques. Tideglusib inhibits GSK-3 irreversibly by presenting a non-competitive inhibition pattern with respect to ATP. The binding of tideglusib seems to directly relate to the motif containing Cys199.

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