Zhang, Heng; Song, Qing; Yu, Guangjun; Cao, Zhongcheng; Qiang, Xiaoming; Liu, Xiuxiu; Deng, Yong published the artcile< Phthalimide-(N-alkylbenzylamine) cysteamide hybrids as multifunctional agents against Alzheimer's disease: Design, synthesis, and biological evaluation>, HPLC of Formula: 531-88-4, the main research area is Alzheimer disease amino acid BBB AChE anitioxidant human; Alzheimer’s disease; acetylcholinesterase inhibition; anti-Aβ aggregation; antioxidant; multi-target agents; neuroprotective effect; phthalimide-(N-alkylbenzylamine)cysteamide hybrids.
The complex pathogenesis of Alzheimer’s disease (AD) calls for multi-target approach for disease treatment. Herein, based on the MTDLs strategy, a series of phthalimide-(N-alkylbenzylamine) cysteamide hybrids were designed, synthesized, and investigated in vitro for the purpose. Most of the target compounds were found to be potential multi-target agents. In vitro results showed that compound 9e was the representative compound in this series, endowed with high EeAChE and HuAChE inhibitory potency (IC50 = 1.55μM and 2.23μM, resp.), good inhibitory activity against self-induced Aβ1-42 aggregation (36.08% at 25μM), and moderate antioxidant capacity (ORAC-FL value was 0.68 Trolox equivalent). Mol. docking studies rationalized the binding mode of 9e in both PAS and CAS of AChE. Moreover, 9e displayed excellent ability to against H2O2-induced PC12 cell injury and penetrate BBB. Overall, these results highlighted that compound 9e was an effective and promising multi-target agent for further anti-AD drug development.
Chemical Biology & Drug Design published new progress about Alzheimer disease. 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, HPLC of Formula: 531-88-4.
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem