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Synthesis of benzimidazole and benzothiazole derivatives as a sirtuins 2 inhibitor / 药学学报
Acta Pharmaceutica Sinica ; (12): 773-778, 2017.
Article in Zh | WPRIM | ID: wpr-779657
Responsible library: WPRO
ABSTRACT
A series of novel benzimidazole and benzothiazole derivatives were designed and synthesized as inhibitors of SIRT1-SIRT3. The target compounds were synthesized from potassium O-ethyldithiocarbonate through a three-step route. The structures of the obtained compounds were elucidated by 1H NMR and HR-MS. Of all compounds, six showed potent SIRT2-inhibitory activities with IC50 values ranging from 2.8 to 21.2 μmol·L-1. Among them, compound 10c displayed the most potent SIRT2-inhibitory activities (IC50 = 2.8 μmol·L-1), with more than 35-fold selectivity over SIRT1 and SIRT3 (IC50>100 μmol·L-1).
Key words
Full text: 1 Database: WPRIM Language: Zh Journal: Acta Pharmaceutica Sinica Year: 2017 Document type: Article
Full text: 1 Database: WPRIM Language: Zh Journal: Acta Pharmaceutica Sinica Year: 2017 Document type: Article
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