Modification of the anticestodal drug 5-chloro-N-(2-chloro-4-nitrophenyl)- 2-hydroxybenzamide with a view to improve its biological effect

Abstract

Reactions of 5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide, the active substance of the drug Niclosamide (Phenasal), with higher amines (dodecan-1-amine, hexadecan-1-amine) and 1-(2-aminoethyl)-piperazine lead to the formation of the corresponding water-soluble ammonium salts with retention of pharmacophoric groups responsible for the antihelminthic effect, whereas no nucleophilic aromatic substitution of chlorine is observed. The product structure was determined by X-ray analysis. © 2014 Pleiades Publishing, Ltd