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

João Neres; Pascal Bonnet; Philip Edwards; Pravin Kotian; Alejandro Buschiazzo; Pedro Alzari; Richard Bryce; Kenneth Douglas

doi:10.1016/j.bmc.2006.12.024

Journal articles

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

João Neres ¹ Pascal Bonnet ¹ Philip Edwards ¹ Pravin Kotian ² Alejandro Buschiazzo ³ Pedro Alzari ³ Richard Bryce ¹ Kenneth Douglas ^{1, *}

* Corresponding author

1 University of Manchester [Manchester]

2 BioCryst Pharmaceuticals

3 Biochimie Structurale

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.

Document type :

Journal articles

Domain :

Life Sciences [q-bio] / Biochemistry, Molecular Biology / Biomolecules [q-bio.BM]

Life Sciences [q-bio] / Biochemistry, Molecular Biology

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

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

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