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Synthesis, Cruzain Docking, and in vitro Studies of Aryl-4-Oxothiazolylhydrazones Against Trypanosoma cruzi

✍ Scribed by Ana Cristina Lima Leite; Diogo Rodrigo de M. Moreira; Marcos V. de O. Cardoso; Marcelo Zaldini Hernandes; Valéria R. Alves Pereira; Ricardo O. Silva; Alice C. Kiperstok; Milena da S. Lima; Milena B. P. Soares

Publisher
John Wiley and Sons
Year
2007
Tongue
English
Weight
273 KB
Volume
2
Category
Article
ISSN
1860-7179

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✦ Synopsis

Abstract

Research in recent years has demonstrated that the Trypanosoma cruzi cysteine protease cruzain (TCC) is a valid chemotherapeutic target. Herein we describe a small library of aryl‐4‐oxothiazolylhydrazones that have been tested in assays against T. cruzi cell cultures. The docking studies carried out suggest that these compounds are potential ligands for the TCC enzyme. The most promising compound of this series, N‐(4‐oxo‐5‐ethyl‐2′‐thiazolin‐2‐yl)‐N′‐phenylthio‐(Z)‐ethylidenehydrazone (6 f), was shown to be very active at non‐cytotoxic concentrations in in vitro assays with mammalian cells and has a potency comparable with reference drugs such as nifurtimox (Nfx) and benznidazole (Bdz).

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