Synthesis, in vitro and in vivo giardicidal activity of nitrothiazole-NSAID chimeras displaying broad antiprotozoal spectrum.

Blanca Colín-Lozano,Ismael León-Rivera,Manuel Jesús Chan-Bacab,Benjamín Otto Ortega-Morales,Rosa Moo-Puc,Vanessa López-Guerrero,Emanuel Hernández-Núñez,Raúl Argüello-Garcia,Thomas Scior,Elizabeth Barbosa-Cabrera,Gabriel Navarrete-Vázquez

Bioorganic & Medicinal Chemistry Letters（2017）

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摘要

•Five nitrothiazole-NSAID chimeras were designed as antiparasitic compounds.•Compounds 1, 3 and 4 showed potent giardicidal activities in the in vitro assay.•Compound 4 performed an ED50=1.70μg/kg in the in vivo mouse model.•Hybrids showed broad antiprotozoal activity (Leishmania, Trichomonas, Trypanosoma).

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关键词

Antiparasitic,Nitazoxanide,Drug discovery,In vivo,Giardia

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