Synthesis and anticonvulsant evaluation of some new 2-substituted-3- arylpyrido[2,3-d]pyrimidinones

Article abstract of DOI:10.1016/j.bmc.2004.07.068

A series of 2-substituted-3-arylpyrido[2,3-d]pyrimidinones was prepared for evaluation as potential anticonvulsants. In murine screening, compounds 4a-c having a 2-oxo-2-(4-pyridyl)ethyl group in the 2-position and a 2-substituted phenyl moiety at the 3-position of the pyridopyrimidinone system displayed the most potent anti-seizure activity in both the maximal electroshock (MES) and pentylenetetrazol (scPTZ) tests at doses in the 3-10 mg/kg range. Compound 4c showed no agonist activity at the GABA_A receptor and was unable to block presynaptic sodium and calcium channels in vitro.