Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds.


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 muM, 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-beta-cyclodextrins formulation showed a 7.5 times increase in oral bioavailability.


PubMed ID: 28064141

Projects: NMTrypI - New Medicines for Trypanosomatidic Infections

Publication type: Journal

Journal: Eur J Med Chem

Citation: Eur J Med Chem. 2017 Jan 27;126:1129-1135. doi: 10.1016/j.ejmech.2016.12.017. Epub 2016 Dec 9.

Date Published: 27th Jan 2017

Registered Mode: by PubMed ID

Authors: C. Borsari, N. Santarem, J. Torrado, A. I. Olias, M. J. Corral, C. Baptista, S. Gul, M. Wolf, M. Kuzikov, B. Ellinger, G. Witt, P. Gribbon, J. Reinshagen, P. Linciano, A. Tait, L. Costantino, L. H. Freitas-Junior, C. B. Moraes, P. Bruno Dos Santos, L. M. Alcantara, C. H. Franco, C. D. Bertolacini, V. Fontana, P. Tejera Nevado, J. Clos, J. M. Alunda, A. Cordeiro-da-Silva, S. Ferrari, M. P. Costi

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Created: 22nd Jul 2020 at 17:05

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