Design, synthesis and biological evaluation of WC-9 analogs as antiparasitic agents.
Design, synthesis and biological evaluation of WC-9 analogs as antiparasitic agents.
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作为抗寄生虫剂的 WC-9 类似物的设计、合成和生物学评价。
DOI：
10.1016/j.ejmech.2013.09.009
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发表时间：
2013
影响因子：
6.7
通讯作者：
Rodriguez,JuanB
中科院分区：
文献类型：
--
作者：
Elicio,PabloD;Chao,MaríaN;Galizzi,Melina;Li,Catherine;Szajnman,SergioH;Docampo,Roberto;Moreno,SilviaNJ;Rodriguez,JuanB
As a part of our project pointed at the search of new safe chemotherapeutic and chemoprophylactic agents against parasitic diseases, several compounds structurally related to 4-phenoxyphenoxyethyl thiocyanate (WC-9), which were modified at the terminal aromatic ring, were designed, synthesized and evaluated as antiproliferative agents against Trypanosoma cruzi, the parasite responsible of American trypanosomiasis (Chagas disease) and Toxoplasma gondii, the etiological agent of toxoplasmosis. Most of the synthetic analogs exhibited similar antiparasitic activity being slightly more potent than the reference compoundWC-9. For example, the nitro derivative13showed an ED50value of 5.2 μM. Interestingly, the regioisomer ofWC-9, compound36showed similar inhibitory action thanWC-9indicating thatpara-phenyl substitution pattern is not necessarily required for biological activity. The biological evaluation againstT. gondiiwas also very promising. The ED50values corresponding for13,36and37were at the very low micromolar level against tachyzoites ofT. gondii.
