Ontology highlight
ABSTRACT:
SUBMITTER: Eidam O
PROVIDER: S-EPMC3166525 | biostudies-literature | 2010 Nov
REPOSITORIES: biostudies-literature
Eidam Oliv O Romagnoli Chiara C Caselli Emilia E Babaoglu Kerim K Pohlhaus Denise Teotico DT Karpiak Joel J Bonnet Richard R Shoichet Brian K BK Prati Fabio F
Journal of medicinal chemistry 20101101 21
We investigated a series of sulfonamide boronic acids that resulted from the merging of two unrelated AmpC β-lactamase inhibitor series. The new boronic acids differed in the replacement of the canonical carboxamide, found in all penicillin and cephalosporin antibiotics, with a sulfonamide. Surprisingly, these sulfonamides had a highly distinct structure-activity relationship from the previously explored carboxamides, high ligand efficiencies (up to 0.91), and K(i) values down to 25 nM and up to ...[more]