Synthesis and antiinflammatory activity of 4-amino-2-aryl-5-cyano-6-{3- and 4-(N-phthalimidophenyl)} pyrimidines

Falcão, Emerson Peter da Silva; Melo, Sebastião J. de; Srivastava, Rajendra M.; Catanho, Maria Tereza Jansen de A.; Nascimento, Silène Carneiro do

doi:10.1016/j.ejmech.2005.09.009

Cited by 81 publications

(13 citation statements)

References 16 publications

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“…All compounds were suspended in 1% carboxymethylcellulose (CMC) and single dose of 250 mg/Kg was administered intraperitoneally, in the morning [18]. Other animal group received 1% CMC.…”

Section: Methodsmentioning

confidence: 99%

Synthesis and Anti-Inflammatory Activity of New Alkyl-Substituted Phthalimide 1H-1,2,3-Triazole Derivatives

Assis

Silva

Oliveira

et al. 2012

The Scientific World Journal

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Four new 1,2,3-triazole phthalimide derivatives with a potent anti-inflammatory activity have been synthesized in the good yields by the 1,3-dipolar cycloaddition reaction from N-(azido-alkyl)phthalimides and terminal alkynes. The anti-inflammatory activity was determined by injecting carrageenan through the plantar tissue of the right hind paw of Swiss white mice to produce inflammation. All the compounds 3a–c and 5a–c exhibited an important anti-inflammatory activity; the best activity was found for the compounds 3b and 5c, which showed to be able to decrease by 69% and 56.2% carrageenan-induced edema in mice. These compounds may also offer a future promise as a new anti-inflammatory agent.

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“…All compounds were suspended in 1% carboxymethylcellulose (CMC) and single dose of 250 mg/Kg was administered intraperitoneally, in the morning [18]. Other animal group received 1% CMC.…”

Section: Methodsmentioning

confidence: 99%

Synthesis and Anti-Inflammatory Activity of New Alkyl-Substituted Phthalimide 1H-1,2,3-Triazole Derivatives

Assis

Silva

Oliveira

et al. 2012

The Scientific World Journal

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“…Pyrimidine, being an integral part of DNA and RNA, have imparts diverse biological activity viz. anticancer [ 13 , 14 ], antiviral [ 15 , 16 ] antiprotozoal [ 17 ], antihypertensive [ 18 ], antihistaminic [ 19 ], anti-inflammatory [ 20 ], central nervous activities [ 21 ], antibacterial [ 22 , 23 ], antifungal [ 24 , 25 ] and in particular antiangiogenic agents [ 26 ]. Specifically, disubstituted pyrimidines have shown potent anticancer activity as CDK inhibitors [ 27 ], TNF-α inhibitors [ 28 ], Abl tyrosine protein kinase inhibitors [ 29 ], PI-3 kinase inhibitors [ 30 ], Akt kinase inhibitors [ 31 ], and cytokines inhibitors [ 32 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, anti-angiogenic and DNA cleavage studies of novel N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)piperidine-4-carboxamide derivatives

Vinaya

Chandrashekara²,

Rekha³

et al. 2017

Chemistry Central Journal

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A series of novel N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)piperidine-4-carboxamide derivatives 10(a–f), 12(a–c) and 14(a–c) were synthesized and characterized by FTIR, 1H-NMR, mass spectral and elemental analysis. The efficacy of these derivatives to inhibit in vivo angiogenesis was evaluated using chick chorioallantoic membrane (CAM) model and their DNA cleavage abilities were evaluated after incubating with calf thymus DNA followed by gel electrophoresis. These novel piperidine analogues efficiently blocked the formation of blood vessels in vivo in CAM model and exhibited differential migration and band intensities in DNA binding/cleavage assays. Among the tested compounds 10a, 10b, 10c, 12b, 14b and 14c showed significant anti-angiogenic and DNA cleavage activities compared to their respective controls and the other derivatives used in this study. These observations suggest that the presence of electron donating and withdrawing groups at positions 2, 3 and 4 of the phenyl ring of the side chain may determine their potency and as anticancer agents by exerting both anti-angiogenic and cytotoxic effects.

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“…Dihydropyrimidine and their derivatives have attracted increasing interest owing to their therapeutic and pharmaceutical properties, such as antiviral, antitubercular [12], [13], antimicrobial agent [14], [15], [16], [17], [18] antagonists of the human adenosine A2A receptor [19], cyclooxygenase-2 inhibitory activity [20], [21], tyrosine kinase inhibitors, antiamoebic activity [22], [23], cytotoxicity [24], [25] and acetyl cholinesterase inhibitor activity [26]. The discovery during the 1930s that a dihydropyridine (dihydronicotinamide derivative, NADH), “hydrogen-transferring coenzyme” consequently became important in biological system, has generated numerous studies on the biochemical properties of dihydropyridines and their bioisosteres dihydropyrimidines.…”

Section: Introductionmentioning

confidence: 99%

Acetylcholinesterase enzyme inhibitor activity of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines

Elumalai

Ali

Elumalai

et al. 2015

Biotechnology Reports

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A new series of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines was prepared by reacting of N-(3-oxobutanoyl)pyrazine-2-carboxamide with urea/thiourea and appropriate aldehyde in the presence of catalytic amount of laboratory made p-toluenesulfonic acid as an efficient catalyst. Confirmation of the chemical structure of the synthesized compounds (4a–l) was substantiated by TLC, different spectral data IR, 1H NMR, mass spectra and elemental analysis. The synthesized compounds were evaluated for acetyl and butyl cholinesterase (AChE and BuChE) inhibitor activity. The titled compounds exhibited weak, moderate or high AChE and BuChE inhibitor activity. Especially, compound (4l) showed the best AChE and BuChE inhibitory activity of all the 1,2,3,4-tetrahydropyrimidine derivatives, with an IC50 value of 0.11 μM and 3.4 μM.

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Synthesis and antiinflammatory activity of 4-amino-2-aryl-5-cyano-6-{3- and 4-(N-phthalimidophenyl)} pyrimidines

Cited by 81 publications

References 16 publications

Synthesis and Anti-Inflammatory Activity of New Alkyl-Substituted Phthalimide 1H-1,2,3-Triazole Derivatives

Synthesis and Anti-Inflammatory Activity of New Alkyl-Substituted Phthalimide 1H-1,2,3-Triazole Derivatives

Synthesis, anti-angiogenic and DNA cleavage studies of novel N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)piperidine-4-carboxamide derivatives

Acetylcholinesterase enzyme inhibitor activity of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines

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