作者:Stefânia N. Lavorato、Mariana C. Duarte、Daniela P. Lage、Carlos A. P. Tavares、Eduardo A. F. Coelho、Ricardo J. Alves
DOI:10.1007/s00044-017-1805-1
日期:2017.5
We describe herein the antileishmanial activity of 1,3-bis(aryloxy)propan-2-amines, prepared in four simple steps from epichlorohydrin. Among the evaluated compounds, three (4o, 4q, and 4r) displayed considerable activity against Leishmania amazonensis promastigote forms, with IC50 values below 10 µM. We also analyzed the effects of the nature and the position of ring substituent on activity. Two amines
我们在这里描述了从表氯醇四个简单步骤制备的1,3-双(芳氧基)丙-2-胺的抗衰老活性。在所评估的化合物中,三个(4o,4q和4r)显示出对亚马逊利什曼原虫前鞭毛体形式的相当大的活性,IC 50值低于10 µM。我们还分析了环取代基的性质和位置对活性的影响。两种胺(4m和4o)在处理被亚马逊菌感染的巨噬细胞时表现出出色的特性,在测试浓度下将寄生虫负担降低了95%以上。