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3,4,5-三取代异恶唑的合成及抗原虫活性。

Synthesis and Antiprotozoal Profile of 3,4,5-Trisubstituted Isoxazoles.

机构信息

Departamento de Química, Universidade Estadual de Maringá (UEM), Maringá, Brazil.

Departamento de Ciências Básicas da Saúde, Universidade Estadual de Maringá (UEM), Maringá, Brazil.

出版信息

ChemistryOpen. 2021 Oct;10(10):931-938. doi: 10.1002/open.202100141. Epub 2021 Jul 30.

DOI:10.1002/open.202100141
PMID:34331350
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8485799/
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.

摘要

一系列 60 种 4-氨甲基-5-芳基-3-取代异恶唑通过一种有效的方法合成，并在体外对引起被忽视的热带病利什曼病和恰加斯病的原虫——亚马逊利什曼原虫和克氏锥虫进行了评估。13 种化合物表现出大于 10 的选择指数。带有联噻吩核心的 3-N-酰基腙异恶唑衍生物系列表现出最好的抗寄生虫作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ae36/8485799/1bbab1e17d0e/OPEN-10-931-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ae36/8485799/03d1122da047/OPEN-10-931-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ae36/8485799/3630dfe20dfd/OPEN-10-931-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ae36/8485799/42df1546193e/OPEN-10-931-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ae36/8485799/1bbab1e17d0e/OPEN-10-931-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ae36/8485799/03d1122da047/OPEN-10-931-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ae36/8485799/3630dfe20dfd/OPEN-10-931-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ae36/8485799/42df1546193e/OPEN-10-931-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ae36/8485799/1bbab1e17d0e/OPEN-10-931-g006.jpg

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[1]
Synthesis and Antiprotozoal Profile of 3,4,5-Trisubstituted Isoxazoles.

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引用本文的文献

[1]
Hydroxyalkyne-Bithiophene Derivatives: Synthesis and Antileishmanial Activity.

Chem Biol Drug Des. 2025-8

本文引用的文献

[1]
Development of methodologies for the regioselective synthesis of four series of regioisomer isoxazoles from β-enamino diketones.

RSC Adv. 2018-1-25

[2]
Antileishmanial assessment of isoxazole derivatives against .

RSC Med Chem. 2020-7-20

[3]
Novel arylcarbamate-N-acylhydrazones derivatives as promising BuChE inhibitors: Design, synthesis, molecular modeling and biological evaluation.

Bioorg Med Chem. 2021-2-15

[4]
Efficient synthesis and antitumor evaluation of 4-aminomethyl-N-arylpyrazoles: Discovery of potent and selective agents for ovarian cancer.

Bioorg Med Chem. 2021-1-1

[5]
Antiparasitic Behavior of Trifluoromethylated Pyrazole 2-Amino-1,3,4-thiadiazole Hybrids and Their Analogues: Synthesis and Structure-Activity Relationship.

Front Pharmacol. 2020-10-7

[6]
Antiparasitic activities of novel pyrimidine N-acylhydrazone hybrids.

Drug Dev Res. 2021-4

[7]
Recent Advancement in the Search of Innovative Antiprotozoal Agents Targeting Trypanothione Metabolism.

ChemMedChem. 2020-12-15

[8]
-Alkyl Hydroxamates Display Potent and Selective Antileishmanial Activity.

J Med Chem. 2020-5-26

[9]
The synthetic and therapeutic expedition of isoxazole and its analogs.

Med Chem Res. 2018

[10]
1,2-Addition to trifluoromethylated β-enamino diketones: regioselective synthesis of trifluoromethyl-containing azomethine pyrazoles and isoxazoles.

Org Biomol Chem. 2020-4-1

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