Organic Chemistry

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


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.


Thumbnail image of ChemRXIV2.pdf
download asset ChemRXIV2.pdf 0.76 MB [opens in a new tab]

Supplementary material

Thumbnail image of Supplementary info GouinS.pdf
download asset Supplementary info GouinS.pdf 4 MB [opens in a new tab]
Supplementary info GouinS