Ontology highlight
ABSTRACT:
SUBMITTER: Morandi S
PROVIDER: S-EPMC2396669 | biostudies-literature | 2008 Feb
REPOSITORIES: biostudies-literature
Morandi Stefania S Morandi Federica F Caselli Emilia E Shoichet Brian K BK Prati Fabio F
Bioorganic & medicinal chemistry 20071107 3
Boronic acids have proved to be promising selective inhibitors of beta-lactamases, acting as transition state analogues. Starting from a previously described nanomolar inhibitor of AmpC beta-lactamase, three new inhibitors were designed to gain interactions with highly conserved residues, such as Asn343, and to bind more tightly to the enzyme. Among these, one was obtained by stereoselective synthesis and succeeded in placing its anionic group into the carboxylate binding site of the enzyme, as ...[more]