Synthesis and SAR of novel benzoxaboroles as a new class of β-lactamase inhibitors

…, F Rock, M Mohan, M Meewan, SJ Baker, S Lux…

文献索引：Xia, Yi; Cao, Kathy; Zhou, Yasheen; Alley; Rock, Fernando; Mohan, Manisha; Meewan, Maliwan; Baker, Stephen J.; Lux, Sarah; Ding, Charles Z.; Jia, Guofeng; Kully, Maureen; Plattner, Jacob J. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 8 p. 2533 - 2536

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被引用次数: 37

摘要

A new class of benzoxaborole β-lactamase inhibitors were designed and synthesized. 6- Aryloxy benzoxaborole 22 inhibited AmpC P99 and CMY-2 with Ki values in the low nanomolar range. Compound 22 restored antibacterial activity of ceftazidime against Enterobacter cloacae P99 expressing AmpC, a class C β-lactamase enzyme. The SAR around the arylbenzoxaboroles, which included the influence of linker and substitutions ...