Aromatic guanyl hydrazones: Synthesis, structural studies and in vitro activity against Trypanosoma cruzi

A series of 22 aromatic guanyl hydrazones, prepared by condensation of several aldehydes with aminoguanidine hydrochloride, were fully characterized by NMR techniques and tested in vitro against the trypomastigote form of Trypanosoma cruzi, the causative agent of Chagas disease. Most of the compound...

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Published inBioorganic & medicinal chemistry letters Vol. 5; no. 24; pp. 3079 - 3084
Main Authors Messeder, J.C., Tinoco, L.W., Figueroa-Villar, J.D., Souza, E.M., Santa Rita, R., de Castro, S.L.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 21.12.1995
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Summary:A series of 22 aromatic guanyl hydrazones, prepared by condensation of several aldehydes with aminoguanidine hydrochloride, were fully characterized by NMR techniques and tested in vitro against the trypomastigote form of Trypanosoma cruzi, the causative agent of Chagas disease. Most of the compounds, especially those without hydrogen bonding groups and possessing ortho-substitution, were significantly more active than crystal violet (ID 50 536 μM). The most active compound has an ID 50 value of 17 μM (25 times more potent than gentian violet). A series of aromatic guanyl hydrazones were prepared, characterized by NMR techniques, and tested in vitro against the blood forms of T. cruzi.
ISSN:0960-894X
1464-3405
DOI:10.1016/0960-894X(95)00541-5