Synthesis of 2-hydrazolyl-4-thiazolidinones based on multicomponent reactions and biological evaluation against Trypanosoma Cruzi.
Synthesis of 2-hydrazolyl-4-thiazolidinones based on multicomponent reactions and biological evaluation against Trypanosoma Cruzi.
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基于多组分反应的 2-肼基-4-噻唑烷酮合成和针对克氏锥虫的生物学评价。
DOI：
10.1111/j.1747-0285.2010.01071.x
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发表时间：
2011
影响因子：
3
通讯作者：
Mahler,SGraciela
中科院分区：
文献类型：
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作者：
Pizzo,Chiara;Saiz,Cecilia;Talevi,Alan;Gavernet,Luciana;Palestro,Pablo;Bellera,Carolina;Blanch,LuisBruno;Benítez,Diego;Cazzulo,JuanJ;Chidichimo,Agustina;Wipf,Peter;Mahler,SGraciela
合成了18个新的2-羟基-4-噻唑烷酮-5-羧酸、酰胺和5，6-α，β不饱和酯类化合物，并测定了它们的体外抗鞭毛虫活性。在酶测定中，有些试剂在37 μm浓度下表现出活性。使用计算工具和对接将生物反应与化合物的物理化学参数及其克鲁兹痛抑制作用相关联。
A series of 18 novel 2‐hydrazolyl‐4‐thiazolidinones‐5‐carboxylic acids, amides and 5,6‐α,β‐unsaturated esters were synthesized, and theirin vitroactivity on cruzipain andT. cruziepimastigotes was determined. Some agents show activity at 37 μmconcentration in the enzyme assay. Computational tools and docking were used to correlate the biological response with the physicochemical parameters of the compounds and their cruzipain inhibitory effects.