Detalle Publicación


Discovery of new organoselenium compounds as antileishmanial agents

Autores: Al-Tamimi, A. M. S. ; Etxebeste Mitxeltorena, Mikel; Sanmartín Grijalba, Carmen; Jimenez-Ruiz, A.; Syrjanen, L. ; Parkkila, S. ; Selleri, S.; Carta, F. (Autor de correspondencia); Angeli, A. (Autor de correspondencia); Supuran, C. T. (Autor de correspondencia)
Título de la revista: BIOORGANIC CHEMISTRY
ISSN: 0045-2068
Volumen: 86
Páginas: 339 - 345
Fecha de publicación: 2019
We report new organoselenium compounds bearing the sulfonamide moiety as effective inhibitors of the beta-isoform of Carbonic Anhydrase from the unicellular parasitic protozoan L. donovani chagasi. All derivatives were evaluated in vitro for their leishmanicidal activities against Leishmania infantum amastigotes along with their cytotoxicities in human THP-1 cells. Compounds 3e-g showed their activity in the low micromolar range with IC50 values spanning from 0.72 to 0.81 mu M and selectivity indexes (SI) > 8 (for 3g SI > 30), thus much higher than those observed for the reference drugs miltefosine and edelfosine. This is the first study which reports new selenoderivatives with promising leishmanicidal properties and acting as Carbonic Anhydrase inhibitors too thus paving the way to the development of innovative agents for the treatment of neglected diseases such as leishmaniasis.