Synthesis and Antiprotozoal Profile of 3,4,5‐Trisubstituted Isoxazoles
| Autor: | Mariellen Guilherme dos Santos, Celso Vataru Nakamura, Karlos Eduardo Pianoski, Julia Poletto, Samara Mendes de Souza Melo, Sidnei Moura, Michael J. V. da Silva, Danielle Lazarin-Bidóia, Fernanda A. Rosa, Hélito Volpato |
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| Rok vydání: | 2021 |
| Předmět: |
medicine.drug_class
Trypanosoma cruzi media_common.quotation_subject Art history Cover Profile Structure-Activity Relationship parasitic diseases cyclocondensation reactions medicine ANTILEISHMANIAL DRUGS Humans Leishmaniasis QD1-999 media_common Full Paper General Chemistry Art Full Papers Full paper Chemistry antileishmanial drugs Antiprotozoal isoxazoles Cover (algebra) N-acylhydrazone derivatives antiprotozoal agents |
| Zdroj: | ChemistryOpen ChemistryOpen, Vol 10, Iss 10, Pp 931-938 (2021) ChemistryOpen, Vol 10, Iss 10, Pp 930-930 (2021) |
| ISSN: | 2191-1363 |
| DOI: | 10.1002/open.202100141 |
| Popis: | 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. Sixty new 3,4,5‐trisubstituted isoxazole derivatives were synthesized using a straightforward method, and their antiprotozoal profile against promastigote form of L. amazonensis and epimastigote form of T. cruzi were evaluated. The series of 3‐N‐acylhydrazone isoxazoles bearing the bithiophene core exhibited better antiparasitic effects than 3‐carboxyethyl or 3‐carbohydrazide isoxazole analogues. |
| Databáze: | OpenAIRE |
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