کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371190 981839 2011 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and SAR of novel benzoxaboroles as a new class of β-lactamase inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and SAR of novel benzoxaboroles as a new class of β-lactamase inhibitors
چکیده انگلیسی

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 was also established.

A new class of benzoxaborole β-lactamase inhibitors is described. 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.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 8, 15 April 2011, Pages 2533–2536
نویسندگان
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