Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 8, Pages 2533-2536Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.02.024
Keywords
beta-lactamase inhibitors; Benzoxaborole; Antibacterial
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A new class of benzoxaborole beta-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 beta-lactamase enzyme. The SAR around the arylbenzoxaboroles, which included the influence of linker and substitutions was also established. (C) 2011 Elsevier Ltd. All rights reserved.
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