Bioorganic & Medicinal Chemistry 2007-03-01

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

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

Index: Bioorg. Med. Chem. 15 , 2106-19, (2007)

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Abstract

Benzoic acid and pyridine derivatives inhibit recombinant trans-sialidase from Trypanosoma cruzi with I50 values between 0.4 and 1mM. 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.