Polyvalent transition-state analogues of sialyl substrates strongly inhibit bacterial sialidases.

2020 · doi:10.26434/chemrxiv.13013291.v2
preprint OA: closed CC-BY-NC-ND-4.0
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Abstract

Conjugation of the transitionstate-cation analogue DANA to polymeric scaffolds led to highly potent inhibitors of bacterial sialidases. Each clustered DANA on the polymers saw its inhibitory potency for S. pneumoniae or B. thetaiotaomicron sialidases improved by more than four orders of magnitude. This extends the multivalent concept to this important class of enzymes.

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License: CC-BY-NC-ND-4.0