The synthesis and SAR of rhodanines as novel class C beta-lactamase inhibitors

E B Grant; D Guiadeen; E Z Baum; B D Foleno; H Jin; D A Montenegro; E A Nelson; K Bush; D J Hlasta

doi:10.1016/s0960-894x(00)00444-3

The synthesis and SAR of rhodanines as novel class C beta-lactamase inhibitors

Bioorg Med Chem Lett. 2000 Oct 2;10(19):2179-82. doi: 10.1016/s0960-894x(00)00444-3.

Authors

E B Grant¹, D Guiadeen, E Z Baum, B D Foleno, H Jin, D A Montenegro, E A Nelson, K Bush, D J Hlasta

Affiliation

¹ Antimicrohial Agents Research, The R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869, USA. egrant@prius.jnj.com

PMID: 11012024
DOI: 10.1016/s0960-894x(00)00444-3

Abstract

Beta-lactam antibiotics such as the cephalosporins and penicillins have diminished clinical effectiveness due to the hydrolytic activity of diverse beta-lactamases, especially those in molecular classes A and C. A structure activity relationship (SAR) study of a high-throughput screening lead resulted in the discovery of a potent and selective non-beta-lactam inhibitor of class C beta-lactamases.

MeSH terms

Drug Evaluation, Preclinical
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology
Molecular Structure
Piperacillin / antagonists & inhibitors
Piperacillin / pharmacology
Rhodanine / analogs & derivatives*
Rhodanine / chemical synthesis
Rhodanine / chemistry
Rhodanine / pharmacology
Structure-Activity Relationship
beta-Lactamase Inhibitors*
beta-Lactamases / classification

Substances

Enzyme Inhibitors
beta-Lactamase Inhibitors
Rhodanine
beta-Lactamases
Piperacillin