Research developments in the syntheses, anti-inflammatory activities and structure–activity relationships of pyrimidines
Top Cited Papers
Open Access
- 3 February 2021
- journal article
- review article
- Published by Royal Society of Chemistry (RSC) in RSC Advances
- Vol. 11 (11), 6060-6098
- https://doi.org/10.1039/d0ra10657g
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.Funding Information
- Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (Finance Code 001, 88881.311799/2018-01)
- Conselho Nacional de Desenvolvimento Científico e Tecnológico (420852/2018-2)
- Fundação de Apoio ao Desenvolvimento do Ensino, Ciência e Tecnologia do Estado de Mato Grosso do Sul (036/2017 PPSUS-MS (59/300.074/2017))
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