ARTÍCULO

Tellurides bearing sulfonamides as novel inhibitors of leishmanial carbonic anhydrase with potent antileishmanial activity

Autores: Angeli, A. (Autor de correspondencia); Etxebeste Mitxeltorena, Mikel; Sanmartín Grijalba, Carmen; Espuelas Millán, María Socorro; Moreno Amatria, Esther; Azqueta Oscoz, Amaya; Parkkila, S.; Carta, F.; Supuran, C. T. (Autor de correspondencia)
Título de la revista: JOURNAL OF MEDICINAL CHEMISTRY
ISSN: 0022-2623
Volumen: 63
Número: 8
Páginas: 4306 - 4314
Fecha de publicación: 2020
Lugar: WOS
Resumen:
We report for the first time a novel series of tellurides bearing sulfonamide as selective and potent inhibitors of the beta-class carbonic anhydrase (CA; EC 4.2.1.1) enzyme expressed in Leishmania donovani protozoa. Such derivatives showed high activity against axenic amastigotes, and among them, compound 5g (4-(((3,4,5-trimethoxyphenyl)tellanyl)methyl)benzenesulfonamide) showed an IC50 of 0.02 mu M being highly selective for the parasites over THP-1 cells with a selectivity index of 300. The in vitro and in vivo toxicity experiments showed compound 5g to possess a safe profile and thus paving the way for tellurium-containing compounds as novel drug entities.