Synthesis, Structure, and Analgesic Activity of Picolylamides of 2-Hydroxy-4-Oxo-4H-Pyrido-[1,2-a]Pyrimidine-3-Carboxylic Acids

Abstract

With the aim of establishing a structure-analgesic activity relationship, a series of picolylamides of 2-hydroxy-4-oxo-4H-pyrido[1,2-a]-pyrimidine-3-carboxylic acids were synthesized. The characteristics of the spatial structure of this group of substances were assessed. The results of pharmacological studies identified compounds in the study series with marked analgesic properties. However, it was noted that the transition from 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamides to the structurally similar pyrido[1,2-a]pyrimidine derivatives was generally accompanied by some decrease in analgesic activity.