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Phenoxyacetohydrazones against Trypanosoma cruzi
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2021-07-27 , DOI: 10.1007/s00044-021-02768-9
Camila Capelini 1, 2 , Edson F. da Silva 1 , Samir A. Carvalho 1 , Kátia R. de Souza 2 , Juliana M. C. Barbosa 3 , Kelly Salomão 3 , Policarpo A. Sales Junior 4 , Silvane M. F. Murta 4 , Solange M. S. V. Wardell 5 , James L. Wardell 6
Affiliation  

Herein, we reported the design, synthesis, antitrypanosomal and cytotoxic evaluation of a new phenoxyacetohydrazones series. All derivatives were assayed against bloodstream trypomastigote forms of T. cruzi (Y strain) and intracellular amastigotes using the model of L-929 cells infected with trypomastigotes of the Tulahuen strain. Compound (E)-N′-(3.4-dihydroxybenzylidene)-2-phenoxyacetohydrazide (11) showed activity against trypomastigotes (IC50/24 h = 10.3 µM) equivalent to that of benznidazole and with selectivity index (SI) = 46. Against infected cultures, (E)-N′-((5-nitrofuran-2-yl) methylene)-2-phenoxyacetohydrazide (19) was active at the nanomolar range (IC50/96 h = 40 nM), being about 38-fold more active than the standard drug and with SI equal to 2500. Thus, derivatives 11 and 19 could be considered a good prototypes for the development of new candidates for Chagas disease therapy.



中文翻译:

苯氧乙酰腙对抗克氏锥虫

在此,我们报告了一种新的苯氧基乙酰腙系列的设计、合成、抗锥虫和细胞毒性评估。使用被Tulahuen菌株的锥鞭毛体感染的 L-929 细胞模型,针对血流锥鞭毛体形式的克氏锥虫Y株)和细胞内无鞭毛体检测了所有衍生物。化合物 ( E ) -N '-(3.4-二羟基苯亚甲基)-2-苯氧基乙酰肼(11) 对锥虫的活性 (IC 50 /24 h = 10.3 µM) 与苯并硝唑相当,选择性指数 (SI) = 46。受感染的培养物,( E )- N'-((5-nitrofuran-2-yl) 亚甲基)-2-苯氧基乙酰肼 (19) 在纳摩尔范围内具有活性 (IC 50 /96 h = 40 nM),比标准药物的活性高约 38 倍,并且SI 等于 2500。因此,衍生物 11 和 19 可以被认为是开发南美锥虫病治疗新候选药物的良好原型。

更新日期:2021-07-27
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