5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents
5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents
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DOI：
10.1016/j.bmcl.2016.10.014
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发表时间：
2016-11-15
影响因子：
2.7
通讯作者：
Ojo, Kayode K.
中科院分区：
文献类型：
--
作者：
Huang, Wenlin;Hulverson, Matthew A.;Ojo, Kayode K.
恶性疟原虫钙依赖蛋白激酶4(PfCDPK4)是雄配子体脱出所必需的。抑制PfCDPK4是阻断蚊虫传播疟疾的有效途径。一系列5-氨基吡唑-4-甲酰胺类似物被证明是PfCDPK4的有效抑制剂。这些化合物还能够阻止恶性疟原虫雄配子体的剥离，而对哺乳动物细胞没有明显的毒性。(C)2016爱思唯尔有限公司。保留所有权利。
Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) is essential for the exflagellation of male gametocytes. Inhibition of PfCDPK4 is an effective way of blocking the transmission of malaria by mosquitoes. A series of 5-aminopyrazole-4-carboxamide analogues are demonstrated to be potent inhibitors of PfCDPK4. The compounds are also able to block exflagellation of Plasmodium falciparum male gametocytes without observable toxicity to mammalian cells. (C) 2016 Elsevier Ltd. All rights reserved.