Studies toward the structural optimization of new brazilizone-related trypanocidal 1,3,4-thiadiazole-2-arylhydrazone derivatives |
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Authors: | Carvalho Samir A Lopes Francisco A S Salomão Kelly Romeiro Nelilma C Wardell Solange M S V de Castro Solange L da Silva Edson F Fraga Carlos A M |
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Institution: | Funda??o Oswaldo Cruz, Instituto de Tecnologia em Fármacos - Far-Manguinhos, Laboratório de Síntese IV, 21041-250 Rio de Janeiro, RJ, Brazil. |
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Abstract: | Megazol is a highly active compound against Trypanosoma cruzi, and has become a core structure for the design of new trypanocidal agents. Recently, we have identified the new potent trypanocide agent Brazilizone A, which presents an IC(50) twofold more potent than the prototype megazol. This result has encouraged us to further explore structurally-related 1,3,4-thiadiazole-2-arylhydrazone derivatives, in order to get a better understanding of their structural and antiprotozoal activity relationships. Herein we report the synthesis and trypanocidal profile of thirteen new Brazilizone A analogues, which supported the construction of 3D-QSAR models used for its structural optimization. |
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