Synthesis and Anticonvulsant Activity of Novel 1-Substituted-1,2-dihydro-pyridazine-3,6-diones(Medicinal Chemistry)

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The synthesis and pharmacological evaluation of novel 1-substituted-l,2-dihydro-pyridazine-3,6-diones (4a-I, 5a-j) as potential anticonvulsant agents are described. The compounds were tested in vivo for the anticonvulsant activity. The compound which have maximum protection against MES induced seizures is l-[3-(2-aminophenylamino)-2-hydroxypropyl)-l,2-dihydro-pyridazine-3,6-dione 4h (ED_<50>=44.7mg・kg^<-1> i.p.) l-[2-hy-xy-3-piperazin1-yl-propyl)-l,2-dihydro-pyridazine-3,6-dione 4c (ED_<50>=72mg・kg^<-1> i.p.) and l-[2-hydroxy-3- imidazol-l-yl-propyl)-l,2-dihydro-pyridazine-3,6-dione 4d (ED_<50>=79mg・kg^<-1> i.p.) were also found to have maximum protection against MES induced seizures. Whereas all these compounds failed to protect the animals from subcutaneous pentylenetetrazole (Metrozol) seizure threshold test (sc-Met).
公益社団法人日本薬学会の論文
2003-10-01