A REVIEW ON: DESIGN AND SYNTHESIS OF TRIAZOLE DERIVATIVES AS ? - GLUCOSIDASE INHIBITORS

Pravin B. Akolkar*, S. G. Khange, Jyoti D. Kale and Amol P. Darwade

ABSTRACT

Inhibition of α-glucosidase is an effective strategy for controlling postprandial hyperglycemia in diabetic patients. To identify novel inhibitors of this enzyme, a series of novel (R)-1-(2-(4-bromo-2-methoxyphenoxy)propyl)-4- (4-(trifluoromethyl)phenyl)-1H-1,2, 3-triazole derivatives (8a-d and 10a-e) were synthesized. The structure was confirmed by NMR, mass spectrometry and, in the case of compound 8a, single crystal X-ray crystallography. The α-glucosidase inhibitory activity was studied in vitro. Most derivatives showed significant inhibitory activity against α-glucosidase. Their structure-activity relationship and molecular docking studies were performed to elucidate the active pharmacophore of this enzyme. NMR-H, mass spectrometry and elemental analysis. Cytotoxic activity of synthetic compounds. Finally, molecular docking studies were also performed to understand the mechanism of action and binding methods of these derivatives as possible targets in the aromatase binding pocket.

Keywords: Triazoles, Anticancer, NMR, Thin layer chromatography (TLC), Infrared (IR).