STUDYING RETENTION BEHAVIOR, LIPOPHILICITY AND PHARMACOKINETIC CHARACTERISTICS OF N-SUBSTITUTED PHENYL-2-CHLOROACETAMIDES

Abstract

The biological activity of compounds is mostly determined by its physical and structural characteristics. Among the many molecular descriptors that may indicate a potential biological activity of a compound, lipophilicity occupies the most important place. Since chloroacetamides show a variety of physiological activity, the task of this study was to investigate the potential biological activity of newly synthesized derivatives of selected N-substituted phenyl-2-chloroacetamides. Analysis was performed by thin layer chromatography on reversed phase (RP18 F254s TLC), and the mobile phase consisted of mixtures of water-acetic acid and water-dimethylformamide. By varying the volume fraction of organic modifier chromatographic retention constants, RM0, of the compounds were determined. Тhen RM0 were correlated with the software calculated partition coefficient, log P, as a standard measure of lipophilicity. Also, RM0 were correlated with selected pharmacokinetic parameters: intestinal absorption, HIA, the ability to bind to plasma proteins, PPB, and the distribution through the blood-brain barrier, BBB.