Artigo
Design, synthesis and biological evaluation of new aryl thiosemicarbazone as antichagasic candidates
Fecha
2013-08-27Registro en:
European Journal of Medicinal Chemistry, v. 67, p. 142-151.
0223-5234
1768-3254
10.1016/j.ejmech.2013.04.022
WOS:000325121800016
2-s2.0-84882528324
9734333607975413
0000-0003-4141-0455
Autor
Universidade Estadual Paulista (Unesp)
Universidade do Vale do Paraíba
Universidade de São Paulo (USP)
Resumen
The present work reports on the synthesis, biological assaying and docking studies of a series of 12 aryl thiosemicarbazones, which were planned to act over two main enzymes, cruzain and trypanothione reductase. These enzymes are used as targets of trypanocidal activity in Chagas disease control with a minimal mutagenic profile. Three p-nitroaromatic thiosemicarbazones showed high activity against Trypanosoma cruzi in in vitro assays (IC50 < 57 μM), and no mutagenic profile was observed in micronucleous tests. Although the in vitro inhibition test showed that 10-μM doses of eight compounds inhibited cruzain activity, no correlation was found between cruzain inhibition and trypanocidal activity. © 2013 Elsevier Masson SAS. All rights reserved.
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