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

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.

Benzoic acid and pyridine-carboxylic acid derivatives inhibit trans-sialidase from Trypanosoma cruzi with I50 values between 0.4 and 1 mM. The strongest inhibitors in this structural family were:Figure optionsDownload as PowerPoint slide