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来自……的抗葡萄球菌天然产物线虫素的合成与构效关系

Synthesis and SAR of the antistaphylococcal natural product nematophin from .

作者信息

Wesche Frank, Adihou Hélène, Wichelhaus Thomas A, Bode Helge B

机构信息

Molekulare Biotechnologie, Goethe University Frankfurt, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

present address: Respiratory, Inflammation and Autoimmunity, Innovative Medicines and Early Development, Biotech Unit, AstraZeneca, Pepparedsleden 1, Mölndal 43183, Sweden.

出版信息

Beilstein J Org Chem. 2019 Feb 25;15:535-541. doi: 10.3762/bjoc.15.47. eCollection 2019.

Abstract

The repeated and improper use of antibiotics had led to an increased number of multiresistant bacteria. Therefore, new lead structures are needed. Here, the synthesis and an expanded structure-activity relationship of the simple and antistaphylococcal amide nematophin from and synthetic derivatives are described. Moreover, the synthesis of intrinsic fluorescent derivatives, incorporating azaindole moieties was achieved for the first time.

摘要

抗生素的反复不当使用导致多重耐药菌数量增加。因此,需要新的先导结构。在此,描述了来自[具体来源未给出]的简单抗葡萄球菌酰胺线虫素及其合成衍生物的合成以及扩展的构效关系。此外,首次实现了含氮杂吲哚部分的内在荧光衍生物的合成。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0485/6404511/bf7f07b6f62f/Beilstein_J_Org_Chem-15-535-g002.jpg

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