Synthesis and evaluation of naphthyridine compounds as antimalarial agents.
Synthesis and evaluation of naphthyridine compounds as antimalarial agents.
复制标题
萘啶化合物作为抗疟药的合成和评价。
DOI：
10.1016/j.bmcl.2007.09.044
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发表时间：
2007
影响因子：
2.7
通讯作者：
Kong,Yuliang
中科院分区：
文献类型：
--
作者：
Zhu,Shuren;Zhang,Quan;Gudise,Chandrashekar;Meng,Li;Wei,Lai;Smith,Erika;Kong,Yuliang
Primaquine is the drug of choice for the radical cure of Plasmodium vivax malaria, but possesses serious side effects. In this study novel primaquine analogues were designed and synthesized. Lower toxicity was achieved by reducing or eliminating the tendency of forming chemically reactive and toxic intermediates and metabolites. In vitro and in vivo studies found that synthesized compounds were less toxic than the parent compound primaquine, while preserving the desired antimalarial activity. Some of these compounds possess a therapeutic index over 10 times superior to that of the commonly used antimalarial drug chloroquine. These compounds, as well as the underlying design rationale, may find usefulness in the discovery and development of new antimalarial drugs.
