Synthesis, in vitro α-glucosidase inhibitory activity and molecular docking studies of new thiazole derivatives

Add time:08/22/2019    Source:sciencedirect.com

Current study based on the synthesis of new thiazole derivatives via “one pot” multicomponent reaction, evaluation of their in vitro α-glucosidase inhibitory activities, and in silico studies. All synthetic compounds were fully characterized by 1H NMR, 13C NMR and EIMS. CHN analysis was also performed. These newly synthesized compounds showed activities in the range of IC50 = 9.06 ± 0.10–82.50 ± 1.70 μM as compared to standard acarbose (IC50 = 38.25 ± 0.12 μM). It is worth mentioning that most of the compounds such as 1 (IC50 = 23.60 ± 0.39 μM), 2 (IC50 = 22.70 ± 0.60 μM), 3 (IC50 = 22.40 ± 0.32 μM), 4 (IC50 = 26.5 ± 0.40 μM), 6 (IC50 = 34.60 ± 0.60 μM), 7 (IC50 = 26.20 ± 0.43 μM), 8 (IC50 = 14.06 ± 0.18 μM), 9 (IC50 = 17.60 ± 0.28 μM), 10 (IC50 = 27.16 ± 0.41 μM), 11 (IC50 = 19.16 ± 0.19 μM), 12 (IC50 = 9.06 ± 0.10 μM), 13 (IC50 = 12.80 ± 0.21 μM), 14 (IC50 = 11.94 ± 0.18 μM), 15 (IC50 = 16.90 ± 0.20 μM), 16 (IC50 = 12.60 ± 0.14 μM), 17 (IC50 = 16.30 ± 0.29 μM), and 18 (IC50 = 32.60 ± 0.61 μM) exhibited potent inhibitory potential. Molecular docking study was performed in order to understand the molecular interactions between the molecule and enzyme. Newly identified α-glucosidase inhibitors except few were found to be completely non-toxic.

We also recommend Trading Suppliers and Manufacturers of ALPHA-(4-BROMOPHENYLIMINO)-N,N-DIMETHYL-P-TOLUIDINE (cas 15485-29-7). Pls Click Website Link as below: cas 15485-29-7 suppliers

Prev:Probing the compound (E)-2-[(4-bromophenylimino)methyl]-6-ethoxyphenol mainly from the point of tautomerism in solvent media and the solid state by experimental and computational methods
Next:Full paper/MémoireK2CO3-catalyzed synthesis of 2-amino-3-cyano-4H-chromene derivatives with different substituents in water)