INVESTIGADORES
LABADIE Guillermo Roberto
artículos
Título:
Synthesis and antikinetoplastid activity of a series of N,N´-substituted diamines
Autor/es:
CAMINOS, A. P.; PANOZZO ZENERE, E. A.; WILKINSON, S. R.; TEKWANI, B. L.; LABADIE, G. R.
Revista:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Editorial:
PERGAMON-ELSEVIER SCIENCE LTD
Referencias:
Lugar: Amsterdam; Año: 2012 vol. 22 p. 1712 - 1715
ISSN:
0960-894X
Resumen:
A series of 25 N,N-substituted diamines were prepared by controlled reductive amination of free aliphatic diamines with different substituted benzaldehydes. The library was screened in vitro for antiparasitic activity on the causative agents of human African trypanosomiasis, Chagas disease and visceral leishmaniasis. The most potent compounds were derived from a subset of diamines that contained a 4-OBn substitution, having a 50% parasite growth inhibition in the submicromolar (against Trypanosoma cruzi) or nanomolar (against Trypanosoma brucei and Leishmania donovani) range. We conclude that members of this series of N,N´-substituted diamines provide new lead structures that have potential to treat trypanosomal and leishmanial infections.
