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Benzoic acid and pyridine derivatives as inhibitors of Trypanosoma cruzi trans-sialidase

Abstract : Benzoic acid and pyridine derivatives inhibit recombinant trans-sialidase from Trypanosoma cruzi with I 50 values between 0.4 and 1 mM. The best compounds, 4-acetylamino-3-hydroxymethylbenzoic acid and 5-acetylamino-6-aminopyridine-2-carboxylic acid, provide new leads to inhibitors not containing the synthetically complex sialic acid structure. The weak inhibition by such compounds contrasts with their much stronger inhibition of neuraminidase from Influenza virus.
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Submitted on : Saturday, April 25, 2020 - 12:13:46 AM
Last modification on : Thursday, May 14, 2020 - 1:27:22 AM

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João Neres, Pascal Bonnet, Philip Edwards, Pravin Kotian, Alejandro Buschiazzo, et al.. Benzoic acid and pyridine derivatives as inhibitors of Trypanosoma cruzi trans-sialidase. Bioorganic and Medicinal Chemistry, Elsevier, 2007, 15 (5), pp.2106-2119. ⟨10.1016/j.bmc.2006.12.024⟩. ⟨pasteur-02554109⟩

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