Poster Presenter

Qspr Studies Of Newly Synthesized Succinimide Derivatives
Nada Ugljesa Perisic-Janjic, Natasa Bozickovic, Jovan Popovic, Gorgana Uscumlic
Serbia

Succinimides and their derivatives exhibit anticonvulsant and antimuscarinic activity. Considering the importance of succinimides as bioactive compounds, we studied the properties of two series of newly synthesized succinimide derivatives.

The biological activity of a compounds depend, among factors, on its ability to reach the intended site of action. In many cases this occurs via passive transport which can be modulated by the physicochemical properties of a compound such as lipophilicity (logP) ionization constant (pKa), or solubility(S). Chromatographic techniques enable us to determine the retention constants RM0, which usually characterize well the lipophilicity of compounds. Owing to its simplicity, as well as efficiency, reversed-phase thin-layer chromatography was selected for this investigation.Considering the practical importance of succinimede derivatives, we (i) examine the retention behaviuor in the reversed-phase chromatographic system; (ii) establish relationships between chromatographic data and selected physico-chemical properties that are related to ADME(absorption, distribution, metabolism and elimination). High statistical quality were established between retention constants, RM0 and ChemSilico predictors: Plasma Protein Binding and Human Intestinal Absorption Predictor, separately. It can be stated that, reverse phase RM0 values of the investigated compounds are recommended for expression of the lipophilicity and pharmacokinetic properties due to highly significant correlation with logP and pharmacokinetic predictors.The chromatographic approach has been quite successful in modeling physicochemical and biological processes.