Kavraiskyi D. Experimental study of novel pyrazolo[3,4-d]pyrimidine-4-one and triazole derivatives as potential anticonvulsants

The PhD thesis experimentally justify for the feasibility of creation a novel original anticonvulsant drug containing pyrazolo[3,4-d]pyrimidine-4-one derivative – 1-(4-methoxyphenyl)-5-{2-[4-(4-methoxy-phenyl)piperazine-1-yl]-2-oksoetyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one. Two series of original pyrazolo[3,4-d]pyrimidine-4-one and triazole derivatives were investigated. The "chemical structure – anticonvulsant activity" pattern has been found for them. The absolute leader – 1-(4-methoxyphenyl)-5-{2-[4-(4-methoxy-phenyl)piperazine-1-yl]-2-oksoetyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one was selected among the investigated derivatives. The leader is effective on seizures’ model with different pathogenetic mechanisms, affects the exchange of neuroactive amino acids and serotonin, has targeted impacts on more affected hemisphere and differs according to the mechanism of action of sodium valproate. It was established that this compound has a favorable range of concomitant psychotropic properties, anti-inflammatory and analgesic effects, as well as low toxicity. The detected pharmacophores can be considered as the basis for further chemical modification may contribute to the direct synthesis of new triazole and pyrazolo[3,4-d]pyrimidine-4-one derivatives with anticonvulsive effect.