625848-14-8

Basic information

• Product Name: 5-bromo-3-(4-(trifluoromethyl)phenyl)pyrazin-2-amine
• Synonyms: 5-bromo-3-(4-(trifluoromethyl)phenyl)pyrazin-2-amine
• CAS NO: 625848-14-8
• Molecular Weight: 318.096
• Mol File: 625848-14-8.mol
• Article Data: 7

Chemical Properties

• CAS DataBase Reference: 5-bromo-3-(4-(trifluoromethyl)phenyl)pyrazin-2-amine(CAS DataBase Reference)
• NIST Chemistry Reference: 5-bromo-3-(4-(trifluoromethyl)phenyl)pyrazin-2-amine(625848-14-8)
• EPA Substance Registry System: 5-bromo-3-(4-(trifluoromethyl)phenyl)pyrazin-2-amine(625848-14-8)

Safety Data

• Hazardous Substances Data: 625848-14-8(Hazardous Substances Data)

Upstream product

• 1062608-42-7 5-bromo-3-iodo-2-aminopyrazine 
• 128796-39-4 4-trifluoromethylphenylboronic acid 
• 24241-18-7 2-amino-3,5-dibromopyrazine 

Downstream Products

• 1450666-64-4 5-(4-(methylsulfonyl)phenyl)-3-(4-(trifluoromethyl)phenyl)pyrazin-2-amine 
• 1450666-70-2 5-{4-[(morpholin-4-yl)carbonyl]phenyl}-3-[4-(trifluoromethyl)phenyl]pyrazin-2-amine 
• 625848-38-6 5-(4-[tert-butyl(dimethyl)silyloxy]phenyl)-3-[4'-(trifluoromethyl)phenyl]-2-pyrazinamine 

Relevant articles and documents

NEW ANTI-MALARIAL AGENTS

The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.

Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity

Replacement of the pyridine core of antimalarial 3,5-diaryl-2- aminopyridines led to the identification of a novel series of pyrazine analogues with potent oral antimalarial activity. However, other changes to the pyridine core and replacement or substitution of the 2-amino group led to loss of antimalarial activity. The 3,5-diaryl-2-aminopyrazine series showed impressive in vitro antiplasmodial activity against the K1 (multidrug resistant) and NF54 (sensitive) strains of Plasmodium falciparum in the nanomolar IC50 range of 6-94 nM while also demonstrating good in vitro metabolic stability in human liver microsomes. In the Plasmodium berghei mouse model, this series generally exhibited good efficacy at low oral doses. One of the frontrunner compounds, 4, displayed potent in vitro antiplasmodial activity with IC 50 values of 8.4 and 10 nM against the K1 and NF54 strains, respectively. When evaluated in P. berghei-infected mice, compound 4 was completely curative at an oral dose of 4 × 10 mg/kg.

Pyrazinecarboxamide derivatives as CB1 antagonists

The present invention relates to compounds of the formula I: wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.