Based on the structure of compound B51(IC_(50) = 37.4 μM), which was discovered as hit in a previous virtual screen, a series of methylisoxazole/isothiazole amide derivatives were designed and synthesized as BACE1 inhibitors. The methoxyphenylpyrimidone fragment of B51 was transformed into a methoxyphenylmethylisoxazole/isothiazole moiety to reduce the molecular weight while retaining the ability to fit into the S1' and S2' subpocket of BACE1 as predicted by docking studies. The effects of BACE1 inhibition ...
【基金】
The National Natural Science Foundation of China(Grant No.21002002);
the Beijing Natural Science Foundation(Grant No.7162110)
【更新日期】
2018-04-23
【分类号】
R914;R96
【正文快照】
1.Introduction Alzheimer’s disease(AD)is a neurodegenerativedisease,which affects 20–30 million individuals worldwideand is recognized as the leading cause of dementia[1]characterized by memory loss,cognitive dysfunction,and neurological impairment[2].H
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