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SAR Studies of the Leupyrrins: Design and Total Synthesis of Highly Potent Simplified Leupylogs.
Chemistry - A European Journal ( IF 4.3 ) Pub Date : 2020-07-01 , DOI: 10.1002/chem.202002622
Paul R Wosniok 1, 2 , Christopher Knopf 1, 3 , Sandra Dreisigacker 1, 4 , J Manuel Orozco-Rodriguez 5 , Bettina Hinkelmann 5 , Peter P Mueller 5 , Mark Brönstrup 5 , Dirk Menche 1
Affiliation  

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.

中文翻译:

Leupyrrins的SAR研究:高强度简化Leupylogs的设计和全合成。

亮丙瑞林是高度有效的抗真菌剂。报道了对天然和合成衍生物的结构-活性-关系研究,该研究揭示了对几种结构亚基的生物学相关性的重要见解,从而导致发现了具有稳定且易于获得的芳族侧链的高效但显着简化的亮链木。对于它们的综合,描述了一种简明的策略,该策略允许进行短而通用的访问。
更新日期:2020-07-01
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