Synthesis, characterization, and antimalarial activity of novel Schiff-base-phenol and naphthalene-amine ligands

被引:43
作者
Harpstrite, Scott E. [1 ]
Collins, Silvia D. [1 ]
Oksman, Ana [2 ,3 ]
Goldberg, Daniel E. [2 ,3 ]
Sharma, Vijay [1 ]
机构
[1] Washington Univ, Sch Med, Mallinckrodt Inst Radiol, St Louis, MO 63110 USA
[2] Washington Univ, Howard Hughes Med Inst, Sch Med, St Louis, MO 63110 USA
[3] Washington Univ, Dept Med & Mol Microbiol, Sch Med, St Louis, MO 63110 USA
关键词
naphthalene-amine; Schiff-base phenol; antimalarials; chloroquine-resistance; P; falciparum;
D O I
10.2174/157340608784872280
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Emergence of chloroquine (CQ) resistant Plasmodium falciparum strains necessitates discovery of inexpensive antimalarial drugs capable of targeting CQ-resistant strains. Towards this objective, herein we have synthesized and characterized naphthalene-Schiff bases or naphthalene-amine phenols. Among these compounds, 7 demonstrated a significant bioactivity with a half-maximal inhibitory concentration (IC50) of 1.7 mu M against CQ-resistant Dd2 strains.
引用
收藏
页码:392 / 395
页数:4
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