Development of a Reversed-Phased Thin-Layer Chromatography Method for the Lipophilicity Prediction of 17 beta-Carboxamide Glucocorticoid Derivatives
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Octanol-water partition coefficients (log Po/w) of fifteen previously synthesized 17 beta-carboxamide glucocorticoid derivatives and prednisolone were determined using shake-flask method. The retention behavior of selected compounds was tested in five reversed-phased thin-layer chromatography (RP-TLC) systems, consisting of water and organic solvent (acetonitrile, acetone, ethanol 96%, methanol, or tetrahydrofuran), and chromatography parameters (R-M(0), S, and C-0) were calculated. Simple linear regression (SLR) analysis was performed, and the correlation between log Po/w and chromatography parameters was tested. The most appropriate RP-TLC system for log Po/w prediction was that consisting of water and ethanol 96% as the mobile phase. Statisitical evaluation of the quality of models created using this system proved their reliability for log Po/w prediction of new 17 beta-carboxamide glucocorticoid derivatives, and the model with the most favorable statistical parameters was underline...d.
Keywords:Reversed-phased thin-layer chromatography / 17 beta-Carboxamide glucocorticoid derivatives / log Po/w / Simple linear regression
Source:Journal of Planar Chromatography - Modern TLC, 2018, 31, 3, 250-256
- Akademiai Kiado Zrt, Budapest