Microwave synthesis of disubstituted pyrrolidine-2,5-dione derivatives
Succinimide (pyrrolidine-2,5-dione) derivatives are organic compounds with a broad spectrum of pharmacological activities. Analogs of this cyclic ureide are well-known and comercially available anticonvulsants (ethosuccinimide, metosuccinimide and fensuccinimide), antipsychotics, sedatives, anticanc...
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| Dokumentumtípus: | Könyv része |
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University of Szeged
Szeged
2024
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| Sorozat: | Proceedings of the International Symposium on Analytical and Environmental Problems
30 |
| Kulcsszavak: | Gyógyszerkémia |
| Tárgyszavak: | |
| Online Access: | http://acta.bibl.u-szeged.hu/85753 |
| Tartalmi kivonat: | Succinimide (pyrrolidine-2,5-dione) derivatives are organic compounds with a broad spectrum of pharmacological activities. Analogs of this cyclic ureide are well-known and comercially available anticonvulsants (ethosuccinimide, metosuccinimide and fensuccinimide), antipsychotics, sedatives, anticancer and antiviral agents. In this paper, using a modified microwave procedure, three succinimide derivatives were synthetized and completely structurally characterized by determination of melting points, as well as FT-IR/ATR, 1H NMR, 13C NMR and elemental analysis. The influence of chemical structure on the pharmacological activity of succinimide derivatives was evaluated using the pioneering "rule of five", Veber, Egan, and Ghose’s empirical criteria, as well as using different in silico methods. Obtained values of molecular descriptors were compared with the characteristic values for reference drugs such as methosuccinimide and ethosuccinimide. Calculated molecular descriptors suggest that the investigated compounds fulfill necessary empirical criteria which qualify them as interesting drug candidates. The obtained descriptors indicate a high degree of gastrointestinal absorption (98%) of the synthesized succinimide derivatives. They are expected to successfully pass through the blood-brain barrier due to the adequate lipophilicity. |
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| Terjedelem/Fizikai jellemzők: | 335-339 |
| ISBN: | 978-963-688-009-5 |