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Leupyrrin 的 SAR 研究：高活性简化 Leupylogs 的设计与全合成。

SAR Studies of the Leupyrrins: Design and Total Synthesis of Highly Potent Simplified Leupylogs.

机构信息

Kekulé-Institut für Organische Chemie und Biochemie, Universität Bonn, Gerhard-Domagk-Str. 1, 53121, Bonn, Germany.

Current address: Eurofins Umwelt West GmbH Wesseling, Vorgebirgsstrasse 20, 50389 Wesseling, Germany.

出版信息

Chemistry. 2020 Nov 26;26(66):15074-15078. doi: 10.1002/chem.202002622. Epub 2020 Oct 15.

DOI:10.1002/chem.202002622
PMID:32608026
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7756798/
Abstract

Leupyrrins are highly potent antifungal agents. A structure-activity-relationship study of natural and synthetic derivatives is reported which reveals important insights into the biological relevance of several structural subunits leading to the discovery of highly potent but drastically simplified leupylogs that incorporate a stable and readily available aromatic side chain. For their synthesis a concise strategy is described that enables a short and versatile access.

摘要

莱菔素是一种高效的抗真菌试剂。本文报道了天然和合成衍生物的结构-活性关系研究，揭示了几个结构亚基对生物相关性的重要见解，从而发现了高效但大大简化的莱菔素类似物，其中包含稳定且易于获得的芳香侧链。为了合成这些物质，本文还描述了一种简洁的策略，能够实现短而通用的合成途径。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f83e/7756798/f0e660448378/CHEM-26-15074-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f83e/7756798/f7a6644ca88e/CHEM-26-15074-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f83e/7756798/33fe6f4b5289/CHEM-26-15074-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f83e/7756798/1dd85fd8d885/CHEM-26-15074-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f83e/7756798/848282ded152/CHEM-26-15074-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f83e/7756798/f0e660448378/CHEM-26-15074-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f83e/7756798/f7a6644ca88e/CHEM-26-15074-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f83e/7756798/33fe6f4b5289/CHEM-26-15074-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f83e/7756798/1dd85fd8d885/CHEM-26-15074-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f83e/7756798/848282ded152/CHEM-26-15074-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f83e/7756798/f0e660448378/CHEM-26-15074-g002.jpg

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