Elucidation of the Teixobactin Pharmacophore
نویسندگان
چکیده
منابع مشابه
X-ray crystallographic structure of a teixobactin analogue reveals key interactions of the teixobactin pharmacophore.
The X-ray crystallographic structure of a truncated teixobactin analogue reveals hydrogen-bonding and hydrophobic interactions and a cavity that binds a chloride anion. Minimum inhibitory concentration (MIC) assays against Gram-positive bacteria correlate the observed structure with antibiotic activity.
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To cope with the global bacterial multidrug resistance, scientific communities have devoted significant efforts to develop novel antibiotics, particularly those with new modes of actions. Teixobactin, recently isolated from uncultured bacteria, is considered as a promising first-in-class drug candidate for clinical development. Herein, we report its total synthesis by a highly convergent Ser li...
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ژورنال
عنوان ژورنال: ACS Chemical Biology
سال: 2016
ISSN: 1554-8929,1554-8937
DOI: 10.1021/acschembio.6b00295