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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.; Franco, C.H.; Bertolacini, C.D.; Fontana, V.; Tejera Nevado, P.; Clos, J.; Alunda, J.M.; Cordeiro-da-Silva, A.; Ferrari, S.; Costi, M.P.


European journal of medicinal chemistry 126 (2017), S.1129-1135
ISSN: 0009-4374
ISSN: 0223-5234
ISSN: 1768-3254
Fraunhofer IME ()

Chalcones display a broad spectrum of pharmacological activities. Herein, a series of 2’-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 = 1.3–4.2 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.