Design, synthesis and biological evaluation of 3-[4-(7-chloro-quinolin-4-yl)-piperazin-1-yl]-propionic acid hydrazones as antiprotozoal agents
作者:Afreen Inam、Shadab Miyan Siddiqui、Taís Soares Macedo、Diogo Rodrigo Magalhaes Moreira、Ana Cristina Lima Leite、Milena Botelho Pereira Soares、Amir Azam
DOI:10.1016/j.ejmech.2014.01.023
日期:2014.3
N-Acylhydrazones derived from 7-chloro-4-piperazin-1-yl-quinoline were synthesized and biologically evaluated for blood-stage of Plasmodium falciparum and Entamoeba histolytica trophozoites. N-Acylhydrazone F12 was found to inhibit the P. falciparum growth as well as its life cycle with good selectivity, which was achieved by inhibiting hematin formation. Compound F24 showed better IC50 value than
合成了由7-氯-4-哌嗪-1-基-喹啉衍生的N-酰基hydr,并对其恶性疟原虫和组织解脂Entamoeba滋养体的血液状态进行了生物学评估。Ñ -Acylhydrazone F12被发现抑制恶性疟原虫的生长以及具有很好的选择性,这是通过抑制羟高铁血红素的形成达到了它的生命周期。化合物F24的IC 50值比杀螨药甲硝唑更好。