Planejamento e síntese de novos candidatos a protótipos de fármacos anti-crises epiléticas
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2023-03-06
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Universidade Federal de Goiás
Resumo
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.
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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.