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.

Utilisation of bis-chloroacetamide derivative in the synthesis of new biologically active sulfide compounds

“…It has received remarkable attention as this intermediate features various biological activities (for example, analgesic, antitumor, anti-microbial, antioxidant, hypoglycemic, and antipyretic) and applications in agriculture. [15][16][17][18][19][20][21][22][23][24] Moreover, different 2-chloroacetamide compounds have been utilised in solid-state chemistry 25 and were found to produce pharmacologically favourable compounds. [26][27][28][29] Also, various transformations of chloroacetamide compounds could lead to the preparation of sulfur-containing compounds.…”