Issue 11, 2021

Research developments in the syntheses, anti-inflammatory activities and structure–activity relationships of pyrimidines

Abstract

Pyrimidines are aromatic heterocyclic compounds that contain two nitrogen atoms at positions 1 and 3 of the six-membered ring. Numerous natural and synthetic pyrimidines are known to exist. They display a range of pharmacological effects including antioxidants, antibacterial, antiviral, antifungal, antituberculosis, and anti-inflammatory. This review sums up recent developments in the synthesis, anti-inflammatory effects, and structure–activity relationships (SARs) of pyrimidine derivatives. Numerous methods for the synthesis of pyrimidines are described. Anti-inflammatory effects of pyrimidines are attributed to their inhibitory response versus the expression and activities of certain vital inflammatory mediators namely prostaglandin E2, inducible nitric oxide synthase, tumor necrosis factor-α, nuclear factor κB, leukotrienes, and some interleukins. Literature studies reveal that a large number of pyrimidines exhibit potent anti-inflammatory effects. SARs of numerous pyrimidines have been discussed in detail. Several possible research guidelines and suggestions for the development of new pyrimidines as anti-inflammatory agents are also given. Detailed SAR analysis and prospects together provide clues for the synthesis of novel pyrimidine analogs possessing enhanced anti-inflammatory activities with minimum toxicity.

Graphical abstract: Research developments in the syntheses, anti-inflammatory activities and structure–activity relationships of pyrimidines

Supplementary files

Article information

Article type
Review Article
Submitted
19 Des 2020
Accepted
27 Jan 2021
First published
03 Feb 2021
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2021,11, 6060-6098

Research developments in the syntheses, anti-inflammatory activities and structure–activity relationships of pyrimidines

H. U. Rashid, M. A. U. Martines, A. P. Duarte, J. Jorge, S. Rasool, R. Muhammad, N. Ahmad and M. N. Umar, RSC Adv., 2021, 11, 6060 DOI: 10.1039/D0RA10657G

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