Overcoming drug resistance to heme-targeted antimalarials by systematic side chain variation of 7-chloro-4-aminoquinolines

Overcoming drug resistance to heme-targeted antimalarials by systematic side chain variation of 7-chloro-4-aminoquinolines
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DOI:
10.1021/jm800106u
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发表时间:
2008-04-10
影响因子:
7.3
通讯作者:
Wolf, Christian
Wolf, Christian
中科院分区:
医学1区
文献类型:
--
作者:
Yearick, Kimberly;Ekoue-Kovi, Kekeli;Wolf, Christian

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Systematic variation of the branching and basicity of the side chain of chloroquine yielded a series of new 7-chloro-4-aminoquinoline derivatives exhibiting high in vitro activity against four different strains of P. falciparum. Many of the compounds tested showed excellent potency against chloroquine sensitive and resistant strains. In particular 4b, 5a, 5b, 5d, 17a, and 17b were found to be significantly more potent than chloroquine against the resistant strains Dd2 and FCB.