%0 Journal Article
%T Synthesis, in vitro [Formula: see text]-glucosidase inhibitory activity, and in silico study of (E)-thiosemicarbazones and (E)-2-(2-(arylmethylene)hydrazinyl)-4-arylthiazole derivatives.
%A Ali M
%A Khan KM
%A Salar U
%A Ashraf M
%A Taha M
%A Wadood A
%A Hamid S
%A Riaz M
%A Ali B
%A Shamim S
%A Ali F
%A Perveen S
%J Mol Divers
%V 22
%N 4
%D Nov 2018
%M 29948581
%F 3.364
%R 10.1007/s11030-018-9835-2
%X This study is focused on the identification of thiazole-based inhibitors for the [Formula: see text]-glucosidase enzyme. For that purpose, (E)-2-(2-(arylmethylene)hydrazinyl)-4-arylthiazole derivatives were synthesized in two steps and characterized by various spectroscopic techniques. All derivatives and intermediates were evaluated for their in vitro [Formula: see text]-glucosidase inhibitory activity. Thiosemicarbazones 20 and 35, and cyclized thiazole derivatives 2, 5-11, 13, 15, 21-24, 27-31, and 36-37 showed significant inhibitory potential in the range of [Formula: see text]-[Formula: see text] as compared to standard acarbose ([Formula: see text]). A molecular modeling study was carried out to understand the binding interactions of compounds with the active site of enzyme.