In 2016,Wang, Guangcheng; He, Dianxiong; Li, Xin; Li, Juan; Peng, Zhiyun published 《Design, synthesis and biological evaluation of novel coumarin thiazole derivatives as α-glucosidase inhibitors》.Bioorganic Chemistry published the findings.Category: esters-buliding-blocks The information in the text is summarized as follows:
A new series of coumarin thiazole derivatives 7a-7t were synthesized, characterized by 1H NMR, 13C NMR and element anal., evaluated for their α-glucosidase inhibitory activity. The majority of the screened compounds displayed potent inhibitory activities with IC50 values in the range of 6.24 ± 0.07-81.69 ± 0.39 μM, when compared to the standard acarbose (IC50 = 43.26 ± 0.19 μM). Structure-activity relationship (SAR) studies suggest that the pattern of substitution in the Ph ring is closely related to the biol. activity of this class of compounds Among all the tested mols., compound 7e (IC50 = 6.24 ± 0.07 μM) was found to be the most active compound in the library of coumarin thiazole derivatives Enzyme kinetic studies showed that compound 7e is a non-competitive inhibitor with a Ki of 6.86 μM. Furthermore, the binding interactions of compound 7e with the active site of α-glucosidase were confirmed through mol. docking. This study has identified a new class of potent α-glucosidase inhibitors for further investigation. In the experiment, the researchers used many compounds, for example, Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Category: esters-buliding-blocks)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Category: esters-buliding-blocks
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics