Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity
datasetposted on 09.04.2020, 14:07 by Andrea Angeli, Mikel Etxebeste-Mitxeltorena, Carmen Sanmartín, Socorro Espuelas, Esther Moreno, Amaya Azqueta, Seppo Parkkila, Fabrizio Carta, Claudiu T. Supuran
We report for the first time a novel series of tellurides bearing sulfonamide as selective and potent inhibitors of the β-class carbonic anhydrase (CA; EC 188.8.131.52) 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 μM 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.
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IC 50tellurium-containing compoundscompound 5 gPotent Antileishmanial Activityselectivity indexNovel Inhibitors0.02 μ Mvivo toxicity experimentsSuch derivativesECnovel drug entitiesCAβ- class carbonic anhydraseTHPaxenic amastigotesLeishmanial Carbonic AnhydraseLeishmania donovani protozoaTellurides Bearing Sulfonamidesnovel series