Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 25, Issue 7, Pages 1420-1424Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-016-1580-4
Keywords
Cycloadditions; 1,3-Diazabuta-1,3-dienes; 5-(Isoindole-1,3-dione)-pyrimidinones; Anticonvulsant activities; MES test; scPTZ test
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Funding
- Amritsar College of Engineering and Technology
- Rayat Bahra College of Pharmacy
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The present work involves the synthesis of previously unknown 5-(isoindole-1,3-dione) pyrimidinones by [4 + 2] cycloaddition reactions of functionalized 1,3-diazabuta-1,3-dienes with phthalimidoketene, generated in situ from phthaloylglycine, tosyl chloride, and triethylamine. The 5-(isoindole-1,3-dione)-pyrimidinones have been screened in vivo for their anticonvulsant activities using MES and PTZ methods. A comparative study for in vivo anticonvulsant activities of these functionalized pyrimidinones with a variety of substitutions at different positions was also conducted. 2-(4-Dimethylamino-6-oxo-1,2-diphenyl-1,6-dihydro-pyrimidin-5-yl)-isoindole-1,3 dione has shown the maximum anticonvulsant activities at 100 mg/kg test dose using MES and PTZ tests.
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