A rapid synthesis of low-nanomolar divalent LecA inhibitors in four linear steps from D-galactose pentaacetate

07 juillet 2020 par Super Administrateur [TheChamp-Sharing]
We have just published our results in collaboration with Helmholtz Centre for Infection Research, Deutsches Zentrum für Infektionsforschung (DZIF) and Saarland University, regarding LecA inhibitors in order to fight against Pseudomonas aeruginosa.

Chronic infections with Pseudomonas aeruginosa are associated with the formation of bacterial biofilms. The tetrameric P. aeruginosa lectin LecA is a virulence factor and an anti-biofilm drug target. Increasing the overall binding affinity by multivalent presentation of binding epitopes can enhance the weak carbohydrate–ligand interactions. Low-nanomolar divalent LecA ligands/inhibitors with up to 260-fold valency-normalized potency boost and excellent selectivity over human galectin-1 were synthesized from D-galactose pentaacetate and benzaldehyde-based linkers in four linear steps.

Our publication is availaible here:
https://pubs.rsc.org/en/content/articlehtml/2020/cc/d0cc03490h