Synthesis of novel triazole-linked mefloquine derivatives: Biological evaluation against Plasmodium falciparum
Synthesis of novel triazole-linked mefloquine derivatives: Biological evaluation against Plasmodium falciparum
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DOI：
10.1016/j.bmcl.2014.10.015
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发表时间：
2014-12-01
影响因子：
2.7
通讯作者：
Blackie, Margaret A. L.
中科院分区：
文献类型：
--
作者：
Hamann, Anton R.;de Kock, Carmen;Blackie, Margaret A. L.
以甲氟喹的药效团2，8-二（三氟甲基）喹啉为骨架，应用CuAAC化学方法合成了11个三唑类化合物。然后测定化合物对恶性疟原虫氯喹敏感菌株NF 54的体外生物活性。这些化合物都显示IC（50）在较低μ M范围内，其中（1 R，3S，5 R）- N-{[1-（2，8-二（三氟甲基）喹啉-4-基）-1H-1，2，3-三唑-4-基]甲基}金刚烷-2-胺（29）显示最佳活性，为1.00 μ M。(C)2014爱思唯尔有限公司版权所有。
Using 2,8-bis(trifluoromethyl) quinoline, the pharmacophore of mefloquine, as scaffold, eleven novel triazole-linked compounds have been synthesised by the application of CuAAC chemistry. The in vitro biological activity of the compounds on the Plasmodium falciparum chloroquine-sensitive strain NF54 was then determined. The compounds all showed IC(50)s in the lower mu M range with (1R, 3S, 5R)- N-{[1-( 2,8bis( trifluoromethyl) quinoline-4-yl)-1H-1,2,3-triazol-4-yl] methyl} adamantan-2-amine (29) exhibiting the best activity of 1.00 mu M. (C) 2014 Elsevier Ltd. All rights reserved.