Design, synthesis and biological evaluation of 3-[4-(7-chloro-quinolin-4-yl)-piperazin-1-yl]-propionic acid hydrazones as antiprotozoal agents

被引：58

作者：

Inam, Afreen ^{[1
]}

Siddiqui, Shadab Miyan ^{[1
]}

Macedo, Tais Soares ^{[2
]}

Magalhaes Moreira, Diogo Rodrigo ^{[2
]}

Lima Leite, Ana Cristina ^{[3
]}

Pereira Soares, Milena Botelho ^{[2
,4
]}

Azam, Amir ^{[1
]}

机构：

[1] Jamia Millia Islamia, Dept Chem, New Delhi 110025, India

[2] Fundacao Oswaldo Cruz, Ctr Pesquisas Goncalo Moniz, BR-40296710 Salvador, BA, Brazil

[3] Univ Fed Pernambuco, Ctr Ciencias Saude, Dept Ciencias Farmaceut, BR-50740520 Recife, PE, Brazil

[4] Hosp Sao Rafael, Ctr Biotecnol & Terapia Celular, BR-41253190 Salvador, BA, Brazil

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 75卷

关键词：

Malaria; Amoebiasis; Aminoquinoline; Piperazinyl derivatives; Acylhydrazone; IN-VITRO; PLASMODIUM-FALCIPARUM; ENTAMOEBA-HISTOLYTICA; ANTIMALARIAL ACTIVITY; ANTIAMEBIC ACTIVITIES; MEDICINAL CHEMISTRY; HYBRID MOLECULES; DRUGS; CHLOROQUINE; MALARIA;

D O I：

10.1016/j.ejmech.2014.01.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 the amoebicidal drug metronidazole. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：67 / 76

页数：10

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