Guo, Yong; Hou, Enhua; Ma, Nannan; Liu, Zhiyan; Fan, Jiangping; Yang, Ruige published the artcile< Discovery, biological evaluation and docking studies of novel N-acyl-2-aminothiazoles fused (+)-nootkatone from Citrus paradisi Macf. as potential α-glucosidase inhibitors>, Computed Properties of 112-63-0, the main research area is nootkatone aminothiazole synthesis antidiabetic cytotoxicity glucosidase diabetes; (+)-Nootkatone; Cytotoxicity; Molecular docking; Thiazole; Type-2 diabetes; α-Glucosidase inhibitor.
Nowadays, the discovery and development of α-glucosidase inhibitors from natural products or their derivatives represents an attractive approach. Here we reported studies on a series of novel N-acyl-2-aminothiazoles fused (+)-nootkatone and evaluation for their α-glucosidase inhibitory activities. Most of (+)-nootkatone derivatives exhibited more potent α-glucosidase inhibitory ability than the pos. drug acarbose. In particular, compounds I and II showed the most promising α-glucosidase inhibitory ability with IC50 values of 13.2 and 13.8 μM. I and II also exhibited relatively low cytotoxicities towards normal LO2 cells. Kinetic study indicated that compounds I and II inhibited the α-glucosidase in a noncompetitive manner, and mol. docking results were in line with the noncompetitive characteristics that I and II did not bind to the known active sites (Asp214, Glu276 and Asp349). Based on our findings, these (+)-nootkatone derivatives could be used as antidiabetic candidates.
Bioorganic Chemistry published new progress about Antidiabetic agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Computed Properties of 112-63-0.
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