Synthesis and SAR of novel benzoxaboroles as a new class of ß-lactamase inhibitors.
Bioorg Med Chem Lett
; 21(8): 2533-6, 2011 Apr 15.
Article
in En
| MEDLINE
| ID: mdl-21392987
ABSTRACT
A new class of benzoxaborole ß-lactamase inhibitors were designed and synthesized. 6-Aryloxy benzoxaborole 22 inhibited AmpC P99 and CMY-2 with K(i) values in the low nanomolar range. Compound 22 restored antibacterial activity of ceftazidime against Enterobacter cloacae P99 expressing AmpC, a class C ß-lactamase enzyme. The SAR around the arylbenzoxaboroles, which included the influence of linker and substitutions was also established.
Full text:
1
Database:
MEDLINE
Main subject:
Pyrazines
/
Benzoxazoles
/
Boron Compounds
/
Enzyme Inhibitors
/
Beta-Lactamase Inhibitors
/
Anti-Bacterial Agents
Language:
En
Year:
2011
Type:
Article