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Synthesis and Antiprotozoal Profile of 3,4,5-Trisubstituted Isoxazoles
ChemistryOpen ( IF 2.5 ) Pub Date : 2021-07-30 , DOI: 10.1002/open.202100141 Fernanda Andreia Rosa 1 , Samara Mendes de Souza Melo 1 , Karlos Eduardo Pianoski 1 , Julia Poletto 1 , Mariellen Guilherme Dos Santos 1 , Michael Jackson Vieira da Silva 1 , Danielle Lazarin-Bidóia 2 , Hélito Volpato 2 , Sidnei Moura 3 , Celso Vataru Nakamura 2
ChemistryOpen ( IF 2.5 ) Pub Date : 2021-07-30 , DOI: 10.1002/open.202100141 Fernanda Andreia Rosa 1 , Samara Mendes de Souza Melo 1 , Karlos Eduardo Pianoski 1 , Julia Poletto 1 , Mariellen Guilherme Dos Santos 1 , Michael Jackson Vieira da Silva 1 , Danielle Lazarin-Bidóia 2 , Hélito Volpato 2 , Sidnei Moura 3 , Celso Vataru Nakamura 2
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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.
中文翻译：
3,4,5-三取代异恶唑的合成和抗原虫特性
通过有效的方法合成了一系列 60 种 4-氨基甲基 5-芳基-3-取代异恶唑，并在体外对分别引起被忽视的热带疾病利什曼病和查加斯病的亚马逊利什曼原虫和克氏锥虫进行了体外评价。13种化合物的选择性指数大于10。以联噻吩为核心的3- N-酰基腙异恶唑衍生物系列表现出最好的抗寄生虫效果。
更新日期：2021-10-01
中文翻译：
3,4,5-三取代异恶唑的合成和抗原虫特性
通过有效的方法合成了一系列 60 种 4-氨基甲基 5-芳基-3-取代异恶唑，并在体外对分别引起被忽视的热带疾病利什曼病和查加斯病的亚马逊利什曼原虫和克氏锥虫进行了体外评价。13种化合物的选择性指数大于10。以联噻吩为核心的3- N-酰基腙异恶唑衍生物系列表现出最好的抗寄生虫效果。
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