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. 2018 Nov;22(4):841-861.
doi: 10.1007/s11030-018-9835-2. Epub 2018 May 29.

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

Muhammad Ali  1 , Khalid Mohammed Khan  2   3 , Uzma Salar  1 , Mohammed Ashraf  4 , Muhammad Taha  5 , Abdul Wadood  6 , Sujhla Hamid  4 , Muhammad Riaz  6 , Basharat Ali  1 , Shahbaz Shamim  1 , Farman Ali  1 , Shahnaz Perveen  7
Affiliations

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

Muhammad Ali et al. Mol Divers. 2018 Nov.

Abstract

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.

Keywords: -glucosidase; In silico; In vitro; Structure–activity relationship (SAR); Synthesis.

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