1428958-99-9

Upstream product

• 1428958-93-3 5-methoxy-1-(2-(methylsulfonyl)pyrimidin-4-yl)-2-(naphthalen-2-yl)-1H-benzo[d]imidazole 
• 108-91-8 cyclohexylamine 
• 66-99-9 β-naphthaldehyde 
• 59548-39-9 4-methoxyphenylene-1,2-diamine dihydrochloride 
• 3367-03-1 5-methoxy-2-naphthalen-2-yl-1H-benzoimidazole 
• 1428958-89-7 5-methoxy-1-(2-(methylthio)pyrimidin-4-yl)-2-(naphthalen-2-yl)-1H-benzo[d]imidazole 
• 96-96-8 4-methoxy-2-nitroaniline 

Downstream Products

• 1428959-12-9 1‐(2‐(cyclohexylamino)pyrimidin‐4‐yl)‐2‐(naphthalen‐2‐yl)‐1H‐benzo[d]imidazol‐5‐ol 

Relevant academic research and scientific papers

Discovery of a potent and selective JNK3 inhibitor with neuroprotective effect against amyloid β-induced neurotoxicity in primary rat neurons

As members of the MAPK family, c-Jun-N-terminal kinases (JNKs) regulate the biological processes of apoptosis. In particular, the isoform JNK3 is expressed explicitly in the brain at high levels and is involved in the pathogenesis of neurodegenerative diseases such as Alzheimer’s disease (AD) and Parkinson’s disease (PD). In this study, we prepared a series of five 6-dihydroxy-1H-benzo[d]imidazoles as JNK3 inhibitors and found them have potential as neuroprotective agents. Following a previous lead scaffold, benzimidazole moiety was modified with various aryl groups and hydroxylation, and the resulting compounds exhibited JNK3 inhibitory activity with improved potency and selectivity. Out of 37 analogues synthesized, (S)-cyclopropyl(3-((4-(2-(2,3-dihydro-benzo[b][1,4]dioxin -6-yl)-5,6-dihydroxy-1H-benzo[d]imidazol-1-yl)pyrimidin-2-yl)amino) piperi-din-1-yl)methanone (35b) demonstrated the highest JNK3 inhibition (IC50 = 9.7 nM), as well as neu-roprotective effects against Aβ-induced neuronal cell death. As a protein kinase inhibitor, it also showed excellent selectivity over other protein kinases including isoforms JNK1 (>1000 fold) and JNK2 (–10 fold).

Novel benzoimidazole derivates havig JNK-inhibitory activity and use thereof

The present invention relates to novel benzimidazole derivatives having C-Jun N-terminal kinase (JNK)-inhibitory activities, and relates to a use thereof. According to the present invention, novel benzimidazole derivatives or pharmaceutically acceptable slats thereof exhibit the excellent inhibitory activities in accordance with c-Jun N-terminal kinase 3 (JNK 3), and are expected to treat the target by approaching the prevention or the treatment of degenerative brain diseases in a fundamental manner.COPYRIGHT KIPO 2018

Syntheses and biological evaluation of 1-heteroaryl-2-aryl-1H-benzimidazole derivatives as c-Jun N-terminal kinase inhibitors with neuroprotective effects

1-Heteroaryl-2-aryl-1H-benzimidazole derivatives were synthesized as inhibitors of c-Jun N-terminal kinases, JNK3. Their activities were evaluated through measurement of Kd using SPR, JNK3 kinase assay, and cell-viability of human neuroblastoma