TY  - CONF
PB  - University of Szeged
TI  - Microwave synthesis of disubstituted pyrrolidine-2,5-dione derivatives
SN  - 978-963-688-009-5
ID  - acta85753
M2  - Szeged
T2  - 30th International Symposium on Analytical and Environmental Problems
N1  - Bibliogr.: 339. p. ; ill. ; összefoglalás angol nyelven
N2  - 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.
UR  - http://acta.bibl.u-szeged.hu/85753/
VL  - 30
SP  - 335
AV  - public
Y1  - 2024///
CY  - Szeged
A1  -  Dimitrijevi? Marija
A1  -  Gak Simi? Kristina
A1  -  Ma?ulovi? Aleksandra
A1  -  Matovi? Luka
A1  -  La?arevi? Jelena
A1  -  Banjac Neboj?a
A1  -  Tri?ovi? Nemanja
A1  -  Lazi? Anita
KW  - Gyógyszerkémia
EP  - 339
ER  -