Cao, Zhongcheng; Song, Qing; Yu, Guangjun; Liu, Zhuoling; Cong, Shiqing; Tan, Zhenghuai; Deng, Yong published the artcile< Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease>, Computed Properties of 531-88-4, the main research area is benzylidene benzyl phthalide Mannich base preparation Alzheimers disease treatment; 3-benzylidene/benzylphthalide Mannich base derivatives; AChE inhibitors; Alzheimer’s disease; Antioxidants; MAO-B inhibitors; Multifunctional anti-AD agents.
To discover novel multifunctional agents for the treatment of Alzheimer’s disease, a series of 3-benzylidene/benzylphthalide Mannich base derivatives were designed, synthesized and evaluated. The biol. screening results indicated that most of these derivatives exhibited good multifunctional activities. Among them, compound (Z)-13c (I) raised particular interest because of its excellent multifunctional bioactivities. It displayed excellent EeAChE and HuAChE inhibition (IC50 = 9.18 x 10-5 and 6.16 x 10-4 μM, resp.), good MAO-B inhibitory activity (IC50 = 5.88μM) and high antioxidant activity (ORAC = 2.05 Trolox equivalent). Addnl., it also exhibited good antiplatelet aggregation activity, moderate self- and Cu2+-induced Aβ1-42 aggregation inhibitory potency, disaggregation ability on Aβ1-42 fibrils, biometal chelating ability, appropriate BBB permeability and significant neuroprotective effect. Furthermore, (Z)-13c can also ameliorate the learning and memory impairment induced by scopolamine in mice. These multifunctional properties highlight compound (Z)-13c as a promising candidate for further development of multifunctional drug against AD.
Bioorganic & Medicinal Chemistry published new progress about Alzheimer disease. 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, Computed Properties of 531-88-4.
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem