Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Determination of radical scavenging activities of some pyrimidine derivatives

Oluwole S Aremu¹ , Lebogang Katata-Seru¹, Olukayode O Aremu², Constance R Sewani-Rusike², Neil Koorbanally³

For correspondence:- Oluwole Aremu Email: 23859539@nwu.ac.za Tel:+27842905180

Accepted: 16 October 2019 Published: 31 January 2020

Citation: Aremu OS, Katata-Seru L, Aremu OO, Sewani-Rusike CR, Koorbanally N. Determination of radical scavenging activities of some pyrimidine derivatives. Trop J Pharm Res 2020; 19(1):45-49 doi: 10.4314/tjpr.v19i1.7

© 2020 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..

Abstract

Purpose: To synthesize some pyrimidine derivatives and investigate their radical scavenging activities.

Methods: A series of newly pyranopyrimidines derivatives and dithiopyridopyrimidinediones were synthesized by condensation of barbituric acid, malononitrile and different substituted benzaldehydes reacted with 1,4-Diazabicyclo[2.2.2] octane (DABCO) as a base. Compounds P1-7 (series 1), S1-11 (series 2) Scheme 1 and 6-amino-2-thiouracil with aromatic aldehydes in glacial acetic acid under reflux J1-13 (series 3) Scheme 2. ¹H & ¹³C NMR, CHN, GC-MS and IR were used to characterize the compounds and were also screened for radical scavenging activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity (IC₅₀ = 50 µg/ml).

Results: The potency of radical scavenging activity was ranked as series 1 > series 3 > series 2. Compounds P3, J4, S10, P5, P7 with inhibitory concentration at 50 % level (IC₅₀) of 12, 40, 48, 50, and 54 µg/ml, respectively, showed radical scavenging activity equal or more potent than the standard antioxidant, ascorbic acid (IC₅₀ = 50 µg/ml).

Conclusion: Series of newly pyranopyrimidines and dithiopyridopyrimidinediones derivatives have been successfully synthesized, and they demonstrate good radical scavenging activity.

Keywords: Pyranopyrimidine, Dipyrimidines, Anti-oxidant, DPPH, Ascorbic acid, Radical scavenging