Abstract
Objective: Pyrimidine heterocycles possessing hydroxy group has a unique place in medicinal chemistry and also plays a key role in biological processes. In the biological functions at cellular level pyrimidine plays imperative roles which lead the researchers to design a variety of its derivatives. The aim of the present study was to synthesize the novel set of 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydropyrimidin-2-ol derivatives. These compounds were screened for their analgesic and anti-inflammatory activities.
 Methods: A novel series of 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydro pyrimidin-2-ol derivatives were furnished in two steps starting from 4-fluoro-3-methyl acetophenone through chalcone formation. Human red blood cell membrane stabilization method and carrageenan-induced rat paw edema test were performed for screening in vitro and in vivo anti-inflammatory activity, respectively. Tail-flick technique was performed for screening analgesic activity.
 Results: All the synthesized 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydro pyrimidin-2-ol derivatives were characterized by Fourier-transform infrared spectroscopy,1H nuclear magnetic resonance, mass spectroscopy, and bases of elemental analysis. The result of biological screening revealed that many of the new derivatives were endowed with improved anti-inflammatory and analgesic activities.
 Conclusion: Nature of the substituent played a major role in anti-inflammatory and analgesic activities. The pyrimidine derivative with chlorophenyl substitution exhibited potent anti-inflammatory and analgesic activities. From the results, it was concluded that 6-(4-chlorophenyl)-4-(4-fluoro-3- methyl phenyl)-1,6-dihydropyrimidin-2-ol was the most active compound.
Highlights
Pyrimidine is ubiquitous in nature and found in a large group of biologically active compounds such as nucleic acids, vitamins, and coenzymes
All the synthesized 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydro pyrimidin-2-ol derivatives were characterized by Fouriertransform infrared spectroscopy,1H nuclear magnetic resonance, mass spectroscopy, and bases of elemental analysis
It was concluded that 6-(4-chlorophenyl)-4-(4-fluoro-3methyl phenyl)-1,6-dihydropyrimidin-2-ol was the most active compound
Summary
Pyrimidine is ubiquitous in nature and found in a large group of biologically active compounds such as nucleic acids, vitamins, and coenzymes. They play a key role in the human physiological process. The aromatic ring consists of a lone pair of electrons in the sp hybrid orbital which belongs to the nitrogen atoms in its plane These lone pairs are not needed for aromatic sextet; they are basic in nature similar to pyridine. Pyrimidine heterocycles possessing hydroxyl group have a unique place in medicinal chemistry [2] and plays a key role in biological processes [3]. Pyrimidine derivatives provide a variety of biological activities such as cytotoxic [5], antimalarial [6], antioxidant [7], tyrosinase inhibitory [8], anti-inflammatory [9], cyclin-dependant kinase inhibitors [10], alopecia agent [11], and antibacterial [12]
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