[en] Metallo-ß-lactamases (MBL) are an emerging cause of bacterial resistance to antibiotic treatment. The VIM-2 ß-lactamase is the most commonly encountered MBL in clinical isolates worldwide. Described here are potent and selective small molecule inhibitors of VIM-2 containing the arylsulfonyl-NH-1,2,3-triazole chemotype that potentiate the efficacy of the ß-lactam, imipenem, in E. coli.
Disciplines :
Biochemistry, biophysics & molecular biology
Author, co-author :
Weide, Timo; The Scripps Research Institute
Saldanha, S. Adrian; The Scripps Research Institute
Minond, Dmitriy; The Scripps Research Institute
Spicer, Timothy; The Scripps Research Institute
Fotsing, Joseph; The Scripps Research Institute
Spaargaren, Michael; The Scripps Research Institute
Frère, Jean-Marie ; Université de Liège - ULiège > Centre d'ingénierie des protéines
Bebrone, Carine ; Université de Liège - ULiège > Centre d'Ingénierie des Protéines
Sharpless, Barry; The Scripps Research Institute
Hodder, Peter; The Scripps Research Institute
Fokin, Valery; The Scripps Research Institute
Language :
English
Title :
NH-1,2,3-Triazole-based Inhibitors of the VIM-2 Metallo-β- Lactamase: Synthesis and Structure-Activity Studies
Publication date :
July 2010
Journal title :
ACS Medicinal Chemistry Letters
eISSN :
1948-5875
Publisher :
American Chemical Society, Washington, United States - District of Columbia
