Liu, Wenjie published the artcileDesign, synthesis and biological evaluation of novel coumarin derivatives as multifunctional ligands for the treatment of Alzheimer’s disease, SDS of cas: 73874-95-0, the main research area is coumarin preparation docking antitumor enzyme inhibitor ADME Alzheimer disease; AChE; Alzheimer’s disease; BACE1; Coumarin; GSK-3β.
Herein, a series of novel coumarin derivatives such as I and II [R = 3-pyridinyl, 4-pyridinyl, 2-F-4-pyridinyl, 6-F-3-pyridinyl, 4-FC6H4, 2-(cyclopropylcarbonylamino)-4-pyridinyl, 2-(benzoylamino)-4-pyridinyl] was explored, synthesized, and assessed their inhibitory effects on cholinesterase (AChE, BuChE), GSK-3β, and BACE1. Among these compounds, compound II (R = pyridin-3-yl) displayed the multifunctional profile of targeting the AChE (IC50 = 1.313 ± 0.099μM) with a good selectivity over BuChE (SI = 24.623), GSK-3β (19.30% inhibition at 20μM), BACE1 (IC50 = 1.227 ± 0.112μM), along with moderate HepG2 cytotoxicity, SH-SY5Y cytotoxicity, low HL-7702 cytotoxicity, as well as good blood-brain barrier (BBB) permeability. Kinetic and docking studies indicated that compound II (R = pyridin-3-yl) was a competitive AChE inhibitor. Furthermore, acute toxicity experiments revealed that it was non-toxic at a dosage of 1000 mg/kg. The ADME prediction results indicate that II (R = pyridin-3-yl) has acceptable physicochem. properties. Collectively, these findings demonstrated that compound II (R = pyridin-3-yl) would be a potential multifunctional candidate for AD therapy.
European Journal of Medicinal Chemistry published new progress about Absorption. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, SDS of cas: 73874-95-0.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem