Reversal agent and linker variants of reversed chloroquines: activities against Plasmodium falciparum.
Reversal agent and linker variants of reversed chloroquines: activities against Plasmodium falciparum.
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DOI：
10.1021/jm900972u
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发表时间：
2010-01-28
影响因子：
7.3
通讯作者：
Peyton DH
中科院分区：
文献类型：
--
作者：
Andrews S;Burgess SJ;Skaalrud D;Kelly JX;Peyton DH
We have shown that “Reversed Chloroquine molecules” constructed from chloroquine-like and resistance “reversal agent”-like cores, can be powerful drugs against malaria (J. Med. Chem., 2006, 49, 5623–5). Several Reversed Chloroquines are now presented which probe parameters governing the activities against chloroquine-resistant and chloroquine-sensitive malaria strains. The design is tolerant to linker and reversal agent changes, but a piperazinyl group adjacent to the quinoline, at least for the group of compounds studied here, may be detrimental.
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