Highly efficient syntheses of novel fluorine bearing quinoline-4-carboxylic acids and the related compounds had been achieved from cyclocondensation of 2-amino-5-fluorophenyl glyoxylic acid 1 with benzoyle asetanilide...Highly efficient syntheses of novel fluorine bearing quinoline-4-carboxylic acids and the related compounds had been achieved from cyclocondensation of 2-amino-5-fluorophenyl glyoxylic acid 1 with benzoyle asetanilides 2 in boiling DMF, to give the target 3. Decarboxylation of 3 produced 6-fluoro-2-phenyl-3-(substituted amino)-keto-quinolines 4, while that reaction underwent refluxing, afforded 7-fluoro-1-(aryl)-3-phenyl-pyrrolo[3,4-c] quinoline-2,9-diones 5. Structure of the products has been established from their elemental and spectral analysis. All targets exhibited a high to moderate activity against some Aspergillus fungi as amylolytic agents.展开更多
Novel heteropolycyclic nitrogen systems bearing fluorine substituted pyrazolo[3,4-d] pyrimidine moiety have been synthesis by the interaction between N’-heteroaryl guanidine 4 with polyfunctional π-acceptors in diff...Novel heteropolycyclic nitrogen systems bearing fluorine substituted pyrazolo[3,4-d] pyrimidine moiety have been synthesis by the interaction between N’-heteroaryl guanidine 4 with polyfunctional π-acceptors in different media and condition. The structures of the synthesis compounds were established by spectroscopic analysis and evaluated as antifungal probes in various concentration.展开更多
A new biocidal agents fluorine substituted-3-thioxopyrimidine-5-carbonitriles (2-9) and/or the related fluorine substi- tuted pyrimido (4,5-d) pyrimidines (10-14) were synthesized by the cycloaddition of fluorinated ...A new biocidal agents fluorine substituted-3-thioxopyrimidine-5-carbonitriles (2-9) and/or the related fluorine substi- tuted pyrimido (4,5-d) pyrimidines (10-14) were synthesized by the cycloaddition of fluorinated β- arylidine malo- nonitriles (1a-c) followed by a nucleophilic attack against α,β-bifunctional reagents in different conditions. Structures of the fluorine targets were characterized by their elemental analysis and spectral data (UV, IR, 1H NMR, 13C NMR and mass measurements) and further evaluated as photochemical probe for inhibition of Vitiligo, it was found that compounds 5, 9, 11 and 12 exhibited high potency over the investigated compounds.展开更多
This overview summarizes recent advanced literature surveys on the synthesis of fluorine substituted 1,2,4-triazine containing various functional groups and/or the related hetero-polycyclic nitrogen systems have been ...This overview summarizes recent advanced literature surveys on the synthesis of fluorine substituted 1,2,4-triazine containing various functional groups and/or the related hetero-polycyclic nitrogen systems have been reported. In addition, physical, chemical, and medicinal properties have been evaluated. The presence of fluorinated atoms often improves these properties with an increasing electronegativity. It, also, enhances the stability of formed carbanion and it improves the hydrophobic effects which have good biological activities.展开更多
In search for new antioxidant agents derived from 6-azauracil, the spiro-5-(flurin-9’-yl)-6-azauracil <strong>3</strong> and their <em>N</em>,<em>N</em>-disubstituted-6-azauracils ...In search for new antioxidant agents derived from 6-azauracil, the spiro-5-(flurin-9’-yl)-6-azauracil <strong>3</strong> and their <em>N</em>,<em>N</em>-disubstituted-6-azauracils <strong>4</strong> - <strong>17</strong> have been synthesized using various methods and reaction conditions. Structure of the new synthesized compounds was deduced from elemental analysis and spectral measurements, for example IR, 1H/13C NMR and mass spectroscopy. The antioxidant evaluation of the new targets showed that the activity increases in the order of <strong>8</strong> > <strong>10</strong> > <strong>6</strong> > <strong>7</strong> > <strong>9</strong> in comparison with 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and ascorbic acid as standards.展开更多
文摘Highly efficient syntheses of novel fluorine bearing quinoline-4-carboxylic acids and the related compounds had been achieved from cyclocondensation of 2-amino-5-fluorophenyl glyoxylic acid 1 with benzoyle asetanilides 2 in boiling DMF, to give the target 3. Decarboxylation of 3 produced 6-fluoro-2-phenyl-3-(substituted amino)-keto-quinolines 4, while that reaction underwent refluxing, afforded 7-fluoro-1-(aryl)-3-phenyl-pyrrolo[3,4-c] quinoline-2,9-diones 5. Structure of the products has been established from their elemental and spectral analysis. All targets exhibited a high to moderate activity against some Aspergillus fungi as amylolytic agents.
文摘Novel heteropolycyclic nitrogen systems bearing fluorine substituted pyrazolo[3,4-d] pyrimidine moiety have been synthesis by the interaction between N’-heteroaryl guanidine 4 with polyfunctional π-acceptors in different media and condition. The structures of the synthesis compounds were established by spectroscopic analysis and evaluated as antifungal probes in various concentration.
文摘A new biocidal agents fluorine substituted-3-thioxopyrimidine-5-carbonitriles (2-9) and/or the related fluorine substi- tuted pyrimido (4,5-d) pyrimidines (10-14) were synthesized by the cycloaddition of fluorinated β- arylidine malo- nonitriles (1a-c) followed by a nucleophilic attack against α,β-bifunctional reagents in different conditions. Structures of the fluorine targets were characterized by their elemental analysis and spectral data (UV, IR, 1H NMR, 13C NMR and mass measurements) and further evaluated as photochemical probe for inhibition of Vitiligo, it was found that compounds 5, 9, 11 and 12 exhibited high potency over the investigated compounds.
文摘This overview summarizes recent advanced literature surveys on the synthesis of fluorine substituted 1,2,4-triazine containing various functional groups and/or the related hetero-polycyclic nitrogen systems have been reported. In addition, physical, chemical, and medicinal properties have been evaluated. The presence of fluorinated atoms often improves these properties with an increasing electronegativity. It, also, enhances the stability of formed carbanion and it improves the hydrophobic effects which have good biological activities.
文摘In search for new antioxidant agents derived from 6-azauracil, the spiro-5-(flurin-9’-yl)-6-azauracil <strong>3</strong> and their <em>N</em>,<em>N</em>-disubstituted-6-azauracils <strong>4</strong> - <strong>17</strong> have been synthesized using various methods and reaction conditions. Structure of the new synthesized compounds was deduced from elemental analysis and spectral measurements, for example IR, 1H/13C NMR and mass spectroscopy. The antioxidant evaluation of the new targets showed that the activity increases in the order of <strong>8</strong> > <strong>10</strong> > <strong>6</strong> > <strong>7</strong> > <strong>9</strong> in comparison with 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and ascorbic acid as standards.