Research Article

Synthesis, alpha-Glucosidase, Thymidine phosphorylase, Lipoxygenase Inhibitory Potentials of Thiobarbituric acid analogues and their Molecular docking studies

Volume: 5 Number: 2 December 31, 2020
  • Hayat Ullah
  • Fahad Khan
  • Muhammad Taha
Journal of Ongoing Chemical Research Cover
Journal of Ongoing Chemical Research
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Synthesis, alpha-Glucosidase, Thymidine phosphorylase, Lipoxygenase Inhibitory Potentials of Thiobarbituric acid analogues and their Molecular docking studies

Abstract

We have reacted 2-dioxo-dihydropyrimidine-2,4(1H, 5H)-dione (thiobarbituric acid) with a different aromatic aldehyde in the presence of NaOH to give thiobarbituric acids analogs (1-29) which were characterized by EI-MS and 1H-NMR and subjected for α-glucosidase, thymidine phosphorylase and lipoxygenase inhibition studies. Analog 19 showed good α-glucosidase inhibitory potential with IC50 values of 37.61 ± 0.08 μM, while analogs 3, 6, 7, 9, 13, 15, 16, 18, 21-27 showed good to moderate α-glucosidase inhibitory potential when compared with standard acarbose having IC50 value 38.25±0.12 μM. Three analogs such as analog 20, 21 and 28 showed outstanding thymidine phosphorylase inhibitory potential with IC50 values 18.8, 40 and 6.9 μM respectively when compared with standard 7-deazaxanthine having IC50 value 41.0 ± 1.63 μM. In the case of lipoxygenase all the analogs were found inactive. Molecular docking studies were carried out to understand the binding interaction of the most active compounds.

Keywords

References

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Details

Primary Language

English

Subjects

-

Journal Section

Research Article

Authors

Hayat Ullah This is me
Pakistan

Fahad Khan This is me
Pakistan

Muhammad Taha This is me
Pakistan

Publication Date

December 31, 2020

Submission Date

August 26, 2020

Acceptance Date

-

Published in Issue

Year 2020 Volume: 5 Number: 2

IZ

https://izlik.org/JA76JU75HL