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

• Published in: Chemistry : a European journal Vol. 26; no. 66; p. 15051
• Main Authors: Wosniok, Paul R., Knopf, Christopher, Dreisigacker, Sandra, Orozco‐Rodriguez, J. Manuel, Hinkelmann, Bettina, Mueller, Peter P., Brönstrup, Mark, Menche, Dirk
• Format: Journal Article
• Language: English
• Published: Weinheim Wiley Subscription Services, Inc 26.11.2020
• Subjects: Chemistry; Natural products
• ISSN: 0947-6539; 1521-3765
• DOI: 10.1002/chem.202003845

Invited for the cover of this issue is the group of Dirk Menche at the University of Bonn. The image depicts the natural product leupyrrin A1 and a synthetic leupylog in balance on an IC50 weighing scale. Read the full text of the article at 10.1002/chem.202002622. “The first set of relevant SAR data for the leupyrrins revealed the high importance of the macrocyclic core, a certain flexibility of the diacid fragment, and high tolerance of the side chain. The leupylogs, which are characterized by a substitution of dihydrofuran side chain by a mere aryl substituent, retain the potent biological activity of the parent natural products. ” Read more about the story behind the cover in the Cover Profile and about the research itself on page 15074 ff. (DOI: 10.1002/chem.202002622).