Ye, Chanyuan; Xu, Rui; Cao, Zhongcheng; Song, Qing; Yu, Guangjun; Shi, Yichun; Liu, Zhuoling; Liu, Xiuxiu; Deng, Yong published the artcile< Design, synthesis, and in vitro evaluation of 4-aminoalkyl-1(2H)-phthalazinones as potential multifunctional anti-Alzheimer's disease agents>, Application of C10H10O4, the main research area is aminoalkylphthalazinone preparation cholinesterase inhibitor SAR antioxidant neuroprotective Alzheimer disease; 4-(aminoalkyl)-1(2H)-phthalazinone derivatives; Acetylcholinesterase inhibitors; Alzheimer’s disease; Anti-neuroinflammation; Aβ aggregation inhibitors; Monoamine oxidases inhibitors; Multifunctional agents.
A series of 4-aminoalkyl-1(2H)-phthalazinone derivatives I (R1 = benzyl, 2-methoxybenzyl, 2-dimethylaminobenzyl, 4-dimethylaminobenzyl, ethyl; R2 = Me, Et; R1R2 = -(CH2)5-, -(CH2)2O(CH2)2-, -(CH2)2N(CH3)(CH2)2-; n = 1, 3, 5) was designed and synthesized as potential multifunctional agents for Alzheimer’s disease (AD) treatment. In vitro biol. assay results demonstrated that most synthesized compounds I exhibited significant AChE inhibition, moderate to high monoamine oxidases (MAO) inhibitory potencies and good anti-platelet aggregation abilities. Among them, compound I (R1 = Bn; R2 = Et; n = 3) (II) exhibited the highest inhibitory potencies towards MAO-B and MAO-A (IC50 = 0.7μM and 6.4μM resp.), moderate inhibition towards AChE (IC50 = 8.2μM), and good activities against self- and Cu2+-induced Aβ1-42 aggregation and platelet aggregation. Moreover, II also displayed antioxidant capacity, neuroprotective potency, anti-neuroinfammation and BBB permeability. These excellent results indicated that compound II could be worthy of further studies to be considered as a promising multifunctional candidate for the treatment of AD.
Bioorganic Chemistry published new progress about Alzheimer disease. 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, Application of C10H10O4.
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem