Jun, Joonhong; Baek, Jihyun; Yang, Songyi; Moon, Hyungwoo; Kim, Hyejin; Cho, Hyunwook; Hah, Jung-Mi published the artcile< Discovery of a Potent and Selective JNK3 Inhibitor with Neuroprotective Effect Against Amyloid β-Induced Neurotoxicity in Primary Rat Neurons>, Quality Control of 27841-33-4, the main research area is amyloid beta neurotoxicity Jun terminal kinase inhibitor neuroprotective effect; Alzheimer’s disease (AD); JNK3; SAR; benzimidazole; neurodegenerative diseases; neuroprotection.
As members of the MAPK family, c-Jun-N-terminal kinases (JNKs) regulate the biol. 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 analogs synthesized, (S)-cyclopropyl(3-((4-(2-(2,3-dihydrobenzo[b][1,4]dioxin -6-yl)-5,6-dihydroxy-1H-benzo[d]imidazol-1-yl)pyrimidin-2-yl)amino) piperidin-1-yl)methanone (35b) demonstrated the highest JNK3 inhibition (IC50 = 9.7 nM), as well as neuroprotective 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).
International Journal of Molecular Sciences published new progress about Cell viability. 27841-33-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H12N2O2, Quality Control of 27841-33-4.
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