Produção Nacional
Revisado por pares
Design, synthesis and biological evaluation of new aryl thiosemicarbazone as antichagasic candidates
2013; Elsevier BV; Volume: 67; Linguagem: Inglês
10.1016/j.ejmech.2013.04.022
ISSN1768-3254
AutoresLorena Blau, Renato Farina Menegon, Gustavo Henrique Goulart Trossini, João Vitor Dutra Molino, Drielli Gomes Vital, Regina Maria Barretto Cicarelli, Gabriela Duó Passerini, Priscila Longhin Bosquesi, Chung Man Chin,
Tópico(s)Synthesis and Biological Evaluation
ResumoThe 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.
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