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

2006; Elsevier BV; Volume: 15; Issue: 5 Linguagem: Inglês

10.1016/j.bmc.2006.12.024

1464-3391

João Neres, Pascal Bonnet, Philip N. Edwards, Pravin L. Kotian, Alejandro Buschiazzo, Pedro M. Alzari, Richard A. Bryce, Kenneth T. Douglas,

Biochemical and Molecular Research

Benzoic acid and pyridine derivatives inhibit recombinant trans-sialidase from Trypanosoma cruzi with I50 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.