Departamento de Química, Universidade Estadual de Maringá (UEM), Maringá, Brazil.
Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Departamento de Ciências Básicas da Saúde, Universidade Estadual de Maringá (UEM), Maringá, Brazil.
Drug Dev Res. 2021 Apr;82(2):230-240. doi: 10.1002/ddr.21745. Epub 2020 Sep 30.
In this article, a series of 29 new pyrimidine N-acylhydrazone hybrids were synthesized and evaluated in vitro against Leishmania amazonensis and Trypanosoma cruzi protozoa that cause the neglected diseases cutaneous leishmaniasis and Chagas disease, respectively. Eight of the target compounds showed significant antiprotozoal activities with IC values in 4.3-33.6 μM range. The more active compound 4f exhibited selectivity index greater than 15 and drug-like properties based on Lipinski's rule.
在这篇文章中，合成了一系列 29 种新型嘧啶 N-酰腙杂合体，并对分别引起被忽视的疾病皮肤利什曼病和恰加斯病的利什曼原虫和克氏锥虫原生动物进行了体外评估。目标化合物中有 8 种表现出显著的抗原生动物活性，IC 值在 4.3-33.6 μM 范围内。更具活性的化合物 4f 表现出大于 15 的选择性指数和基于 Lipinski 规则的类药性。
