Following our previous studies in the field of anticonvulsant agents, we planned a one-pot solution-phase parallel synthesis (SPPS) of a small library of new 1,2,3,4-tetrahydroisoquinoline derivatives. The activity against audiogenic seizures in DBA/2 mice of the newly synthesized compounds has also been evaluated.

Following our previous molecular modeling studies we herein report the synthesis of substituted 1,2,3,4-tetrahydroisoquinolinone-4-carboxylic acids in an attempt to obtain new anticonvulsants acting as negative modulators of AMPA-type glutamate receptor. The evaluation of their pharmacological effects demonstrated that some derivatives were able to prevent audiogenic induced seizures in DBA/2 mice.

2,3,4-Tetrahydroisoquinolin-1-ones as Anticonvulsant Agents. -A series of 13 PD00735 analogues of type (IV)/(V) is prepared and their anticonvulsant activities are studied. All of the compounds are less active than PD00735 with (IVb) and (IVc) showing the highest activities. -(GITTO*, R.; FRANCICA, E.; DE SARRO, G.; SCICCHITANO, F.; CHIMIRRI, A.; Chem.