학술논문

New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria
Document Type
article
Source
Journal of the Serbian Chemical Society, Vol 86, Iss 2, Pp 115-123 (2021)
Subject
quinoline
bromobenzyl derivatives
antimalarials
β-hematin inhibitory activity
Chemistry
QD1-999
Language
English
ISSN
0352-5139
1820-7421
20122500
Abstract
Synthesis of novel aminoquinoline derivatives has been accomplished and their activity against malaria strains has been examined. The compounds showed moderate in vitro antimalarial activity against two P. falciparum strains, 3D7 (CQ susceptible clone) and Dd2 (CQ resistant clone). Three aminoquinolines were further examined for antimalarial efficacy in a mouse model using a modified Thompson test. In this model, mice were infected with P. berghei-infected red blood cells, and drugs were administered orally. Antimalarial 3 was found toxic at a dose of 320 (mg/kg)/day in 3/6 mice, however, 2/6 mice of the same group survived through day 31, and one of them was cured.