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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.

DOI:10.3762/bjoc.15.47
PMID:30873237
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6404511/
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/0485/6404511/0c983d82547e/Beilstein_J_Org_Chem-15-535-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0485/6404511/bf7f07b6f62f/Beilstein_J_Org_Chem-15-535-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0485/6404511/840f44ab1dbe/Beilstein_J_Org_Chem-15-535-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0485/6404511/0c983d82547e/Beilstein_J_Org_Chem-15-535-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0485/6404511/bf7f07b6f62f/Beilstein_J_Org_Chem-15-535-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0485/6404511/840f44ab1dbe/Beilstein_J_Org_Chem-15-535-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0485/6404511/0c983d82547e/Beilstein_J_Org_Chem-15-535-g004.jpg

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本文引用的文献

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Chemical language and warfare of bacterial natural products in bacteria-nematode-insect interactions.细菌-线虫-昆虫互作中细菌天然产物的化学语言和战争
Nat Prod Rep. 2018 Apr 25;35(4):309-335. doi: 10.1039/c7np00054e.
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Biosynthesis of the Antibiotic Nematophin and Its Elongated Derivatives in Entomopathogenic Bacteria.
抗生素线虫素及其在昆虫病原细菌中的衍生延长物的生物合成。
Org Lett. 2017 Feb 17;19(4):806-809. doi: 10.1021/acs.orglett.6b03796. Epub 2017 Jan 30.
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Bioactive natural products from novel microbial sources.新型微生物来源的生物活性天然产物。
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Merging chemical ecology with bacterial genome mining for secondary metabolite discovery.将化学生态学与细菌基因组挖掘相结合,以发现次生代谢产物。
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Rhabdopeptides as insect-specific virulence factors from entomopathogenic bacteria.杆状肽作为昆虫病原细菌的昆虫特异性毒力因子。
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Synthesis, characterization, and heterobimetallic cooperation in a titanium-chromium catalyst for highly branched polyethylenes.合成、表征及钛-铬催化剂中双金属协同作用对高度支化聚乙烯的影响
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Spectroscopic study of the ground and excited state prototropic equilibria of 4-azaindole.4-氮吲哚的基态和激发态质子平衡的光谱研究。
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