Synthesis, trypanocidal activity and docking studies of novel quinoxaline-N-acylhydrazones, designed as cruzain inhibitors candidates

…, H Cerecetto, I Aldana, S Pérez-Silanes…

文献索引：Romeiro, Nelilma C.; Aguirre, Gabriela; Hernandez, Paola; Gonzalez, Mercedes; Cerecetto, Hugo; Aldana, Ignacio; Perez-Silanes, Silvia; Monge, Antonio; Barreiro, Eliezer J.; Lima, Lidia M. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 2 p. 641 - 652

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被引用次数: 81

摘要

In this paper, we report the structural design, synthesis, trypanocidal activity and docking studies of novel quinoxaline-N-acylhydrazone (NAH) derivatives, planned as cruzain inhibitors candidates, a cysteine protease essential for the survival of Trypanosoma cruzi within the host cell. The salicylaldehyde N-acylhydrazones 7a and 8a presented IC50 values of the same magnitude order than the standard drug nifurtimox (Nfx), when tested ...