55543-74-3Relevant academic research and scientific papers
A New Series of Salicylic Acid Derivatives as Non-saccharide α-Glucosidase Inhibitors and Antioxidants
Chen, Jiangang,Lu, Wenfang,Chen, Hao,Bian, Xiaoli,Yang, Guangde
, p. 231 - 246 (2019)
In this study, a series of salicylic acid derivatives were designed and synthesized as novel non-saccharide α-glucosidase inhibitors. Biological evaluation indicated that when compared to acarbose, compounds T9, T10, and T32 exhibited a higher potency of α-glucosidase inhibitory activity with IC50 values of 0.15±0.01, 0.086±0.01 and 0.32±0.02mM, respectively. Evaluation of the inhibition kinetics indicated that T9, T10, T32, and acarbose interacted with α-glucosidase in a mixed non-competitive inhibitory manner. Moreover, T9, T10, and T32 statically quenched the fluorescence of α-glucosidase by formation of an inhibitor-α-glucosidase complex. The docking results showed that hydrogen bonds were generated between the test compounds and α-glucosidase. The antioxidant study revealed that compound T10 exhibited a higher antioxidant activity via scavenging 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH), thereby inhibiting lipid peroxidation and the total reduction capacity. In brief, the salicylic acid derivatives identified in this study were promising candidates for development as novel non-saccharide α-glucosidase inhibitors.
Micromolecular non-nucleoside compound as immunomodulator
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Paragraph 0157; 0159; 0061, (2021/06/09)
The invention discloses a structure, a preparation method and application of a micromolecular non-nucleoside targeted CD73 immunomodulator. The structure of the compound is shown as a general formula (I), and R1, R2, R3, R4, R5, X, Y and W groups are defined as in the claims. The compound acts on CD73 protein, blocks the interaction between the CD73 protein and a substrate of the CD73 protein, and can be used for preparing medicines and/or compositions for treating and/or diagnosing cancers, infectious diseases, autoimmune diseases and neurodegenerative diseases.
