Numerous compounds are synthesized and screened for their anticonvulsant activity each year. To make the discovery of new anticonvulsants more rational many investigators identified structural fragments essential for anticonvulsant properties. One of the structural features that play a significant role in relation to antiepileptic activity is an amide function.^1,2 In the course of developing new anticonvulsant agents as well as taking into consideration the above and vital influence of 4-arylpiperazine moieties on anticonvulsant activity of pyrrolidine-2,5-diones differently substituted at 3-positon of succinimide ring,^3,4 in the present studies we have synthesized a library of 1,3-dioxo-1,3-dihydro-2H-isoindole- and 1,3-dioxoocta- hydro-2H-isoindole-2-carboxamides with the 4-arylpiperazine derivatives as an amide function. The structures of compounds obtained are shown on Figure 1.

 Figure 1.

The desired compounds were prepared by condensation of (1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)- or (1,3-dioxooctahydro- 2H-isoindol-2-yl)- acetic acids with the appropriately substituted 4-arylpiperazines, in the presence of the N,N-carbonyldiimidazole (CDI) reagent. The compounds were evaluated for their anticonvulsant activity and neurotoxic properties within the Antiepileptic Drug Development (ADD) Program (Epilepsy Branch, Neurological Disorders Program, National Institute of the Neurological and Communicative Disorders and Stroke (NINCDS), Rockville, USA).⁵

References:

¹ Estrada E., Pena A. Bioorg. Med. Chem. 2000, 8, 2755. ² Wong M.G., Defina J.A., Andrews P.R. J. Med. Chem. 1986, 29, 562. ³ Obniska J., Zagorska A. Il Framaco 2003, 58, 1227. ⁴ Obniska J., Kamiński K., Tatarczyńska E. Pharmacol. Rep. 2006, 58, 207. ⁵ Kupferberg H. J. Epilepsia 1989, 30 (suppl.), 51.

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