Zhang, Jin-He; Xie, Hong-Xu; Li, Yue; Wang, Kai-Ming; Song, Zhiling; Zhu, Kong-Kai; Fang, Lei; Zhang, Juan; Jiang, Cheng-Shi published their research in Bioorganic & Medicinal Chemistry Letters in 2021. The article was titled 《Design, synthesis and biological evaluation of novel (E)-2-benzylidene-N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)hydrazine-1-carboxamide derivatives as α-glucosidase inhibitors》.Computed Properties of C7H6O3 The article contains the following contents:
In this present study, a series of novel I [R = 2,3-(OH)2, 3-OH, 3,4-(OH)2, etc.] against α-glucosidase were designed and synthesized, and their biol. activities were evaluated in vitro and in vivo. Most of the designed analogs exhibited better inhibitory activity than the marketed acarbose, especially the most potent compound I [R = 3,4-(OH)2] with an IC50 value of 9.26 ± 1.84μM. The direct binding of I [R = 3,4-(OH)2] and I [R = 3,5-(OH)2] with α-glucosidase was confirmed by fluorescence quenching experiments, and the kinetic and mol. docking studies revealed that I [R = 3,4-(OH)2] and I [R = 3,5-(OH)2] inhibited α-glucosidase in a non-competitive manner. Cytotoxicity bioassay indicated compounds I [R = 3,4-(OH)2] and I [R = 3,5-(OH)2] were non-toxic towards LO2 and HepG2 at 100μM. Furthermore, both compounds were demonstrated to have in vivo hypoglycemic activity by reducing the blood glucose levels in sucrose-treated rats. After reading the article, we found that the author used 3,5-Dihydroxybenzaldehyde(cas: 26153-38-8Computed Properties of C7H6O3)
3,5-Dihydroxybenzaldehyde(cas: 26153-38-8) is used as a building block in the synthesis of more complex structures. It is also used in the synthesis of terbutaline, which is an important bronchodilator.Computed Properties of C7H6O3
Referemce:
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