کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376507 | 981959 | 2006 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
We report the identification of the sesquiterpene lactones cnicin and cynaropicrin as potent, irreversible inhibitors of the bacterial enzyme MurA. They covalently bind to the thiol group of Cys115. Judging from the structure–activity relationships, we conclude that the unsaturated ester side chain of cynaropicrin and cnicin is of particular importance for the inhibition of MurA. These results provide evidence that MurA is a target protein of SLs with a probably high relevance for their known antibacterial effect.
Certain sesquiterpene lactones are potent inhibitors of the antibacterial target enzyme MurA. We present structure–activity relationships and discuss biological implications.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 21, 1 November 2006, Pages 5605–5609
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 21, 1 November 2006, Pages 5605–5609
نویسندگان
Anke Bachelier, Ralf Mayer, Christian D. Klein,