Planejamento e síntese de novos candidatos a protótipos de fármacos anti-crises epiléticas

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Universidade Federal de Goiás


Epilepsy is a disease that affects about 50 million people worldwide and the worldwide prevalence is estimated at 1% of the population, and of this global rate, about 30% of patients are refractory to pharmacological treatment. In Brazil, 150 thousand new cases are registered per year. Therefore, this study aims at planning and developing new candidates for prototype anti-epileptic seizure drugs that are safer, more effective and that present fewer adverse reactions, or that can be used as a pharmacological tool. In this situation, the work describes the synthesis of compounds analogous to stiripentol. Ring bioisosterism and hybridization strategies were employed in the planning. To obtain the compounds, a synthetic route with four steps was chosen. The intermediate compound was obtained through the aldol condensation method and the final compound was obtained by the Luche reduction method, which obtained an overall yield in the range of 21% to 23%. The synthesized compounds, with the exception of compound LQFM 311, were within the parameters established by Lipinski and Verber. The compounds obtained in the synthesis were purified by recrystallization method employing solvent mixture and the purification of compound LQFM 311 was performed by column adsorption chromatography. All synthesized compounds were characterized by hydrogen nuclear magnetic resonance (¹H NMR) and ¹³C nuclear magnetic resonance (HSQC and HMBC). This demonstrates that the chosen synthetic route was adequate, allowing the development of new drug prototypes.



ROCHA, A. L. B. Planejamento e síntese de novos candidatos a protótipos de fármacos anti-crises epiléticas. 2023. 74 f. Dissertação (Mestrado em Ciências Biológicas) - Universidade Federal de Goiás,Goiânia, 2023.