The diazines: pyridazine, pyrimidine and pyrazine: reactions and synthesis

Joule, J. A.; Mills, K.; Smith, G. Frederick

doi:10.1007/978-1-4899-3222-8_11

Cited by 3 publications

(1 citation statement)

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“…A solution of aromatic aldehyde (0.01 M), methyl ketone (0.012 M) and metformin ([0.015 M] [N-C-N fragment]) in methanol was refluxed for 12 h in the presence of few drops of concentrated hydrochloric acid as catalyst. [ 12 13 ] The product was isolated through the rotary evaporator and recrystallized using a mixture of water and acetone [ Figure 2 ] (80:20).…”

Section: Methodsmentioning

confidence: 99%

Synthesis, characterization and in silico biological activity of some 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines

et al. 2016

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Introduction:As pyrimidine is a basic nucleus in DNA and RNA, it has been found to be associated with diverse biological activities. Pyrimidine derivatives were reported to possess anticonvulsant, antimicrobial, anti-inflammatory, antitumor, and antihistaminic. Recently, our team reported the anti-inflammatory and antimicrobial evaluation of some pyrimidines.Objective:To synthesize, predict and evaluate biological activity of some 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines.Experimental:seven new pyrimidines were synthesized by following the standard procedures using substituted aromatic aldehydes, methyl ketones and metformin. After the biological activity was predicted using PASS, Molinspiration and Osiris property explorer, their anthelmintic activity was evaluated using Pheretima posthuma. The structural assignment of the title compounds (P1-7) has been made on the basis of elemental analysis, infrared, 1H-nuclear magnetic resonance and Mass spectral studies.Results:All the synthesized compounds were found to obey Lipinski's rule. All the synthesized compounds scored good bioactivity values as GPCR ligands and kinase inhibitors. Among the test compounds, P5 was found to be more potent anthelmintic inducing paralysis in 36-48 minutes and death in 40-51 minutes.Conclusion and Recommendation:The synthesized compound (P5) possessing methoxy group at position-4 of the benzene ring located at position-4 of pyrimidine exhibited good anthelmintic activity. The study revealed the necessity of synthesizing many more compounds with other substituents at position-4 of the benzene ring located at position-4 of pyrimidine.

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Section: Methodsmentioning

confidence: 99%

Synthesis, characterization and in silico biological activity of some 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines

et al. 2016

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The synthesis of one H‐2 labeled and two H‐3 labeled leukotriene C4 synthase inhibitors

Bergare

Kingston

Guly

et al. 2020

Labelled Comp Radiopharmac

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As part of a medicinal chemistry program aimed at developing a leukotriene C4 synthase inhibitor for the treatment of asthma, two tritium‐labeled and one stable isotope‐labeled compounds were required. The synthesis of the tritium‐labeled compounds used a standard bromination‐tritiodehalogentation approach. One of the tritium‐labeled compounds was observed to exchange its tritium label slowly with the solvent. The stable isotope‐labeled compound was prepared in seven steps (3% overall yield) from [2H6]acetone in a modification of the route used by medicinal chemistry.

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Synthesis, biological screening and molecular docking studies of novel 4,6-pyrimidine derivatives as EGFR-TK inhibitors

et al. 2016

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The diazines: pyridazine, pyrimidine and pyrazine: reactions and synthesis

Cited by 3 publications

References 167 publications

Synthesis, characterization and in silico biological activity of some 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines

Synthesis, characterization and in silico biological activity of some 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines

The synthesis of one H‐2 labeled and two H‐3 labeled leukotriene C4 synthase inhibitors

Synthesis, biological screening and molecular docking studies of novel 4,6-pyrimidine derivatives as EGFR-TK inhibitors

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