Wang, Lun; Cai, Xiaoying; Shi, Mingsong; Xue, Linlin; Kuang, Shuang; Xu, Ruiling; Qi, Wenyan; Li, Yan; Ma, Xu; Zhang, Ruijia; Hong, Feng; Ye, Haoyu; Chen, Lijuan published the artcile< Identification and optimization of piperine analogues as neuroprotective agents for the treatment of Parkinson's disease via the activation of Nrf2/keap1 pathway>, Formula: C16H22N2O3, the main research area is piperine analog preparation neuroprotective Parkinsons disease treatment; MPTP; Nrf2 activation; Parkinson’s disease; Piperine analogues.
Parkinson’s disease (PD) is a slowly progressive and complex neurodegenerative disorder. Up to date, there are no approved drugs that could slow or reverse the neurodegenerative process of PD. Here, we reported the synthesis of series of piperine analogs and the evaluation of their neuroprotective effects against hydrogen peroxide (H2O2) induced damage in the neuron-like PC12 cells. Among these analogs, I exhibited the most potent protection effect and its underlying mechanism was further investigated. Further results indicated that the ROS scavenging and cytoprotection effect of I might be related to the Nrf2 activation and upregulation of related phase II antioxidant enzymes, such as HO-1 and NQO1. In in vivo study, oral administration (100 mg/kg) of I significantly attenuated PD-associated behavioral deficits in a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced mouse model of PD and protected tyrosine hydroxylase-immunopos. dopaminergic neurons. Our results provided evidence that I might be a promising candidate for Parkinson’s disease treatment.
European Journal of Medicinal Chemistry published new progress about Antiparkinsonian agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Formula: C16H22N2O3.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics