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

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 exh...

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Detalles Bibliográficos
Autores principales: Rosa, Fernanda Andreia, Mendes de Souza Melo, Samara, Pianoski, Karlos Eduardo, Poletto, Julia, dos Santos, Mariellen Guilherme, Vieira da Silva, Michael Jackson, Lazarin‐Bidóia, Danielle, Volpato, Hélito, Moura, Sidnei, Nakamura, Celso Vataru
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2021
Materias:
Full Papers
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8485799/
https://www.ncbi.nlm.nih.gov/pubmed/34331350
http://dx.doi.org/10.1002/open.202100141
Descripción
Sumario: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.

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