Chalcones display a broad spectrum of pharmacological activities. Herein, a series of 2â-hydroxy methoxylated chalcones was synthesized and evaluated towards Trypanosoma brucei, Trypanosoma cruzi and Leishmania infantum. Among the synthesized library, compounds 1, 3, 4, 7 and 8 were the most potent and selective anti-T. brucei compounds (EC50 = 1.3â4.2 μM, selectivity index >10-fold). Compound 4 showed the best early-tox and antiparasitic profile. The pharmacokinetic studies of compound 4 in BALB/c mice using hydroxypropil-β-cyclodextrins formulation showed a 7.5 times increase in oral bioavailability.
Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds / Borsari, C., Santarem, N., Torrado, J., Olías, A.I., Corral, M.J., Baptista, C., Gul, S., Wolf, M., Kuzikov, M., Ellinger, B., Witt, G., Gribbon, P., Reinshagen, J., Linciano, P., Tait, A., Costantino, L., Freitas-Junior, L.H., Moraes, C.B., Bruno Dos Santos, P., Alcântara, L.M., et al.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 126:(2017), pp. 1129-1135. [10.1016/j.ejmech.2016.12.017]
Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds
Borsari, Chiara;Linciano, Pasquale;Tait, Annalisa;Costantino, Luca;Ferrari, Stefania;Costi, Maria Paola
2017
Abstract
Chalcones display a broad spectrum of pharmacological activities. Herein, a series of 2â-hydroxy methoxylated chalcones was synthesized and evaluated towards Trypanosoma brucei, Trypanosoma cruzi and Leishmania infantum. Among the synthesized library, compounds 1, 3, 4, 7 and 8 were the most potent and selective anti-T. brucei compounds (EC50 = 1.3â4.2 μM, selectivity index >10-fold). Compound 4 showed the best early-tox and antiparasitic profile. The pharmacokinetic studies of compound 4 in BALB/c mice using hydroxypropil-β-cyclodextrins formulation showed a 7.5 times increase in oral bioavailability.
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