Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives.
Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives.
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DOI：
10.1021/jm020960r
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发表时间：
2003-01
影响因子：
7.3
通讯作者：
A. Ryckebusch;R. Deprez-Poulain;L. Maes;M. Debreu-Fontaine;E. Mouray;P. Grellier;C. Sergheraert
中科院分区：
文献类型：
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作者：
A. Ryckebusch;R. Deprez-Poulain;L. Maes;M. Debreu-Fontaine;E. Mouray;P. Grellier;C. Sergheraert
合成了三个系列的由1，4-双（3-氨丙基）哌嗪连接基和多种端基组成的单喹啉。我们的目的是证明，在相关的双喹啉，这是第二个喹啉部分，是负责细胞毒性，它不是克服耐药性氯喹（CQ）的绝对要求。其中11个化合物表现出比CQ更高的选择性指数（CC_（50）/IC_（50）活性比），其中1个化合物对伯氏疟原虫感染小鼠有治愈作用。
Three series of monoquinolines consisting of a 1,4-bis(3-aminopropyl)piperazine linker and a large variety of terminal groups were synthesized. Our aim was to prove that in related bisquinoline, it is the second quinoline moiety that is responsible for cytotoxicity and that it is not an absolute requirement for overcoming resistance to chloroquine (CQ). Eleven compounds displayed a higher selectivity index (ratio CC50/IC50 activity) than CQ, and one of them cured mice infected by Plasmodium berghei.