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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.
SEEK ID: https://fairdomhub.org/publications/558
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
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Created: 22nd Jul 2020 at 15:05
Last updated: 8th Dec 2022 at 17:26
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