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Microwave-Assisted Synthesis, Characterization, Docking Studies and Molecular Dynamic of Some Novel Phenyl Thiazole Analogs as Xanthine Oxidase Inhibitor

Microwave-Assisted Synthesis, Characterization, Docking Studies and Molecular Dynamic of Some... A series of novel substituted 2-(4-bromophenyl)-4-phenylthiazole compounds 5a–h were synthesized by a simplified two-step process. First, the selective and effective α-bromination of substituted acetophenone moieties with N-bromo succinamide was done followed by treating of substituted 2-bromo-1-phenylethan-1-one with 4-bromobenzothiamide under microwave irradiation. The structures of the newly synthesized compounds were confirmed by IR, 1H NMR, 13C NMR, mass spectra and C, H, N analysis. Further, all the synthesized compounds 5a–h were evaluated for xanthine oxidase inhibition. Among all the tested compounds, 5f was found to be highly potent (IC50 = 0.100 ± 0.08 µM) followed by 5e (IC50 = 0.145 ± 1.42 µM), compared to the standard allopurinol (IC50 = 0.150 ± 0.07 µM), which is evident from in vitro and in silico analysis. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Journal of the Iranian Chemical Society Springer Journals

Microwave-Assisted Synthesis, Characterization, Docking Studies and Molecular Dynamic of Some Novel Phenyl Thiazole Analogs as Xanthine Oxidase Inhibitor

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References (61)

Publisher
Springer Journals
Copyright
Copyright © Iranian Chemical Society 2022
ISSN
1735-207X
eISSN
1735-2428
DOI
10.1007/s13738-022-02574-z
Publisher site
See Article on Publisher Site

Abstract

A series of novel substituted 2-(4-bromophenyl)-4-phenylthiazole compounds 5a–h were synthesized by a simplified two-step process. First, the selective and effective α-bromination of substituted acetophenone moieties with N-bromo succinamide was done followed by treating of substituted 2-bromo-1-phenylethan-1-one with 4-bromobenzothiamide under microwave irradiation. The structures of the newly synthesized compounds were confirmed by IR, 1H NMR, 13C NMR, mass spectra and C, H, N analysis. Further, all the synthesized compounds 5a–h were evaluated for xanthine oxidase inhibition. Among all the tested compounds, 5f was found to be highly potent (IC50 = 0.100 ± 0.08 µM) followed by 5e (IC50 = 0.145 ± 1.42 µM), compared to the standard allopurinol (IC50 = 0.150 ± 0.07 µM), which is evident from in vitro and in silico analysis.

Journal

Journal of the Iranian Chemical SocietySpringer Journals

Published: Sep 1, 2022

Keywords: Phenyl thiazole microwave synthesis; Xanthine oxidase inhibition; Docking study

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