Synthesis and Antiprotozoal Profile of 3,4,5‐Trisubstituted Isoxazoles

Abstract

Abstract A series of 60 4‐aminomethyl 5‐aryl‐3‐substituted isoxazoles were synthesized by an efficient method and evaluated in vitro against Leishmania amazonensis and Trypanosoma cruzi, protozoa that cause the neglected tropical diseases leishmaniasis and Chagas disease, respectively. Thirteen compounds exhibited a selective index greater than 10. The series of 3‐N‐acylhydrazone isoxazole derivatives bearing the bithiophene core exhibited the best antiparasitic effects.

Keywords

• antileishmanial drugs
• antiprotozoal agents
• cyclocondensation reactions
• isoxazoles
• N-acylhydrazone derivatives