Syntheses of new 3-thiazolyl coumarin derivatives, in vitro α-glucosidase inhibitory activity, and molecular modeling studies.

Abstract

3-Thiazolylcoumarin derivatives 1-14 were synthesized via one-pot two step reactions, and screened for in vitro α-glucosidase inhibitory activity. All compounds showed inhibitory activity in the range of IC50 = 0.12 ± 0.01-16.20 ± 0.23 μM as compared to standard acarbose (IC50 = 38.25 ± 0.12 μM), and also found to be nontoxic. Molecular docking study was carried out in order to establish the structure-activity relationship (SAR) which demonstrated that electron rich centers at one and electron withdrawing centers at the other end of the molecules showed strong inhibitory activity. All the synthesized compounds were characterized by spectroscopic techniques such as EI-MS, HREI-MS, (1)H NMR and (13)C NMR. CHN analysis was also performed.

DOI: 10.1016/j.ejmech.2016.06.037

Cite this paper

@article{Salar2016SynthesesON, title={Syntheses of new 3-thiazolyl coumarin derivatives, in vitro α-glucosidase inhibitory activity, and molecular modeling studies.}, author={Uzma Salar and Muhammad Taha and Khalid M. Khan and Nor Hadiani Ismail and Syahrul Imran and Shahnaz Perveen and Sahib Gul and Abdul Wadood}, journal={European journal of medicinal chemistry}, year={2016}, volume={122}, pages={196-204} }