relation: http://acta.bibl.u-szeged.hu/85753/
title: Microwave synthesis of disubstituted pyrrolidine-2,5-dione derivatives
creator:  Dimitrijević Marija
creator:  Gak Simić Kristina
creator:  Mašulović Aleksandra
creator:  Matović Luka
creator:  Lađarević Jelena
creator:  Banjac Nebojša
creator:  Trišović Nemanja
creator:  Lazić Anita
subject: 01. Természettudományok
subject: 01.04. Kémiai tudományok
description: 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.
publisher: University of Szeged
date: 2024
type: Konferencia vagy workshop anyag
type: NonPeerReviewed
format: part
language: hu
identifier: http://acta.bibl.u-szeged.hu/85753/1/proceedings_of_isaep_2024_335-339.pdf
identifier:    Dimitrijević Marija;  Gak Simić Kristina;  Mašulović Aleksandra;  Matović Luka;  Lađarević Jelena;  Banjac Nebojša;  Trišović Nemanja;  Lazić Anita:   Microwave synthesis of disubstituted pyrrolidine-2,5-dione derivatives.   
language: eng