186534-01-0

Basic information

• Product Name: Pyrazinecarboxylic acid, trimethyl- (9CI)
• Synonyms: Pyrazinecarboxylic acid, trimethyl- (9CI);3,5,6-Trimethylpyrazin-2-carboxylic acid
• CAS NO: 186534-01-0
• Molecular Formula: C₈H₁₀N₂O₂
• Molecular Weight: 166.1772
• Product Categories: GLYCINESCAFFOLD
• Mol File: 186534-01-0.mol
• Article Data: 3

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Pyrazinecarboxylic acid, trimethyl- (9CI)(CAS DataBase Reference)
• NIST Chemistry Reference: Pyrazinecarboxylic acid, trimethyl- (9CI)(186534-01-0)
• EPA Substance Registry System: Pyrazinecarboxylic acid, trimethyl- (9CI)(186534-01-0)

Safety Data

• Hazardous Substances Data: 186534-01-0(Hazardous Substances Data)

Upstream product

• 75907-74-3 2-Pyrazinemethanol,3,5,6-trimethyl 

Downstream Products

• 1332730-39-8 methyl 3,5,6-trimethylpyrazine-2-carboxylate 

Relevant articles and documents

Synthesis and evaluation of novel ligustrazine derivatives as multi-targeted inhibitors for the treatment of Alzheimer's disease

A series of novel ligustrazine derivatives 8a-r were designed, synthesized, and evaluated as multi-targeted inhibitors for anti-Alzheimer's disease (AD) drug discovery. The results showed that most of them exhibited a potent ability to inhibit both ChEs, with a high selectivity towards AChE. In particular, compounds 8q and 8r had the greatest inhibitory abilities for AChE, with IC50 values of 1.39 and 0.25 nM, respectively, and the highest selectivity towards AChE (for 8q, IC50BuChE/IC50 AChE = 2.91 × 106; for 8r, IC50BuChE/IC50 AChE = 1.32 × 107). Of note, 8q and 8r also presented potent inhibitory activities against Aβ aggregation, with IC50 values of 17.36 μM and 49.14 μM, respectively. Further cellular experiments demonstrated that the potent compounds 8q and 8r had no obvious cytotoxicity in either HepG2 cells or SH-SY5Y cells, even at a high concentration of 500 μM. Besides, a combined Lineweaver-Burk plot and molecular docking study revealed that these compounds might act as mixed-type inhibitors to exhibit such effects via selectively targeting both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChEs. Taken together, these results suggested that further development of these compounds should be of great interest.

PYRAZOLOPYRIMIDINE COMPOUNDS AND THEIR USE AS PDE10 INHIBITORS

The present invention relates to a compound represented by formula [I]: wherein: R1 is hydrogen, halogen, lower alkyl or cyano; Ring A is an optionally substituted heterocyclic group; Ring B is an optionally substituted 3 to 6-membered monocyclic group; and Y is optionally substituted amino, optionally substituted cyclic amino, optionally substituted aliphatic 3 to 6-membered monocyclyloxy, optionally substituted lower alkyl or optionally substituted lower alkyl-O-, or a pharmaceutically acceptable salt thereof, and to their use as PDE10 inhibitor.