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Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal agents. 2012
Samir A Carvalho, and
Larisse O Feitosa, and
Márcio Soares, and
Thadeu E M M Costa, and
Maria G Henriques, and
Kelly Salomão, and
Solange L de Castro, and
Marcel Kaiser, and
Reto Brun, and
James L Wardell, and
Solange M S V Wardell, and
Gustavo H G Trossini, and
Adriano D Andricopulo, and
Edson F da Silva, and
Carlos A M Fraga
Instituto de Tecnologia em Fármacos - Farmanguinhos, Fundação Oswaldo Cruz, 21041-250 Rio de Janeiro, RJ, Brazil.
We report herein the synthesis and trypanocidal profile of new (E)-cinnamic N-acylhydrazones (NAHs) designed by exploiting molecular hybridization between the potent cruzain inhibitors (E)-1-(benzo[d][1,3]dioxol-5-yl)-3-(4-bromophenyl)prop-2-en-1-one and (E)-3-hydroxy-N'-((2-hydroxynaphthalen-1-yl)methylene)-7-methoxy-2-naphthohydrazide. These derivatives were evaluated against both amastigote and trypomastigote forms of Trypanosoma cruzi and lead us to identify two compounds that were approximately two times more active than the reference drug, benznidazole, and with good cytotoxic index. Although designed as cruzain inhibitors, the weak potency displayed by the best cinnamyl NAH derivatives indicated that another mechanism of action was likely responsible for their trypanocide action.
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