Synthesis and evaluation of sulfonylurea derivatives as novel antimalarials
Synthesis and evaluation of sulfonylurea derivatives as novel antimalarials
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DOI：
10.1016/j.ejmech.2007.01.001
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发表时间：
2007-06-01
影响因子：
6.7
通讯作者：
Dominguez, Jose N.
中科院分区：
文献类型：
--
作者：
Leon, Caritza;Rodrigues, Juan;Dominguez, Jose N.
我们已经合成了一系列的磺酰脲类药物，并测试了它们的抗疟活性，包括抑制体外发展的氯喹耐药株Plasniodiunifalcipartan，在体外血红蛋白水解，疟原虫色素的形成，并在鼠疟疾伯氏疟原虫的发展。最有效的抗疟化合物是（E）-1-[4-（3-（2，4-二氟苯基）丙烯酰基）苯基]-3-甲苯磺酰脲（22），对培养的恶性疟原虫的IC 50为1.2 μ M。生物学结果表明该衍生物具有相当有效的抗疟活性，但也意味着其活性可能来自未知的机制。事实上，这些化合物可以通过多种机制对抗疟疾寄生虫。(c)2007年Elsevier Masson SAS。All rights reserved.
We have synthesized a series of sulfonylureas and have tested their antimalarial activities, including inhibition of in vitro development of a chloroquine-resistant strain of Plasniodiunifalcipartan, in vitro hemoglobin hydrolysis, hemozoin formation, and development of Plasmodium berghei in murine malaria. The most active antimalarial compound was (E)-1-[4-(3-(2,4-difluorophenyl)acryloyl)phenyl]-3-tosylurea (22) with an IC50 of 1.2 mu M against cultured P. falciparum parasites. Biological results suggest a fairly potent antimalarial activity for this derivative, but also imply that its activity may arise from an unknown mechanism. Indeed, these compounds may act against malaria parasites through multiple mechanisms. (c) 2007 Elsevier Masson SAS. All rights reserved.