Li, Xiaokang published the artcileDiscovery of nitazoxanide-based derivatives as autophagy activators for the treatment of Alzheimer’s disease, SDS of cas: 328-90-5, the publication is Acta Pharmaceutica Sinica B (2020), 10(4), 646-666, database is CAplus and MEDLINE.
The efficacy and discovery of new chem. entities, two series of NTZ-based derivatives I [R1 = H, SMe, SO2Me, etc.; R2 = 2-OH, 3-OH, 4-OH, 2-OAc] and II [R3 = Me, cyclohexyl, 2-MeC6H4, etc.] were designed, synthesized and evaluated as autophagy activator against AD. All compounds I and II were screened by the inhibition of phosphorylation of p70S6K, which was the direct substrate of mammalian target of rapamycin (mTOR) and its phosphorylation level could reflect the mTOR-dependent autophagy level. Among these analogs, compound II [R3 = 3-OAc] exhibited excellent potency in promoting β-amyloid (Aβ) clearance, inhibiting tau phosphorylation, as well as stimulating autophagy both in vitro and in vivo. Compound II [R3 = 3-OAc] could effectively improved the memory and cognitive impairments in APP/PS1 transgenic AD model mice. These results demonstrated that II [R3 = 3-OAc] was a potential candidate for the treatment of AD.
Acta Pharmaceutica Sinica B published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C8H5F3O3, SDS of cas: 328-90-5.
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