Синтез и биологическая активность N-алкил(арил)-4-R-оксо-2-(2-фениламинобензоилгидразоно)бутанамидов

Abstract

First of all, the main task of pharmacy is search for new compounds, including those with high biological activity. Although lots of known compounds have antinociceptive and anti-inflammatory effects, almost all of them have a toxic effect on the gastrointestinal tract and cause a large number of side effects from various organs and systems of the body, since they are non-selective inhibitors of cyclooxygenase enzyme. The relief of pain and inflammatory processes as well the following search for safe and more efficient compounds is the significant task of pharmacology. It was found that hydrazonamides have very effective anti-inflammatory and antinociceptive activity; they will be perspective for following pharmacological screening. Objective: synthesis and study of anti-inflammatory and antinociceptive activity of N-alkyl(aryl)-4-R-4-oxo-2-(2-phenylaminobenzoylhydrazono)butanamides. Materials and methods. We synthesized the compounds investigated by means of classic organic synthesis; their structures were analyzed with IR, NMR 1 H, NMR 13 C spectroscopy and mass spectrometry. We studied the antinociceptive activity on outbred white mice by «hot plate» method, and anti-inflammatory activity on outbred white rats by the model of acute inflammatory edema. Results. N-alkyl(aryl)-4-R-4-oxo-2-(2-phenylaminobenzoylhydrazono)butanamides showed the high antinociceptive activity, several compounds exhibited anti-inflammatory effect. Conclusion. N-alkyl(aryl)-4-R-4-oxo-2-(2-phenylaminobenzoylhydrazono)butanamides have perspective for the following in-depth study, including on acute toxicity and other types of biological activity.