《Discovery of nitazoxanide-based derivatives as autophagy activators for the treatment of Alzheimer’s disease》 was written by Li, Xiaokang; Lu, Jian; Xu, Yixiang; Wang, Jiaying; Qiu, Xiaoxia; Fan, Lei; Li, Baoli; Liu, Wenwen; Mao, Fei; Zhu, Jin; Shen, Xu; Li, Jian. Category: thiazole And the article was included in Acta Pharmaceutica Sinica B in 2020. The article conveys some information:
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. In the experiment, the researchers used 5-Bromothiazol-2-amine(cas: 3034-22-8Category: thiazole)
5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Category: thiazole
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica