The Hydrophobicity and Antifungal Potentiation of Burkholdine Analogues

The Hydrophobicity and Antifungal Potentiation of Burkholdine Analogues

The burkholdines are a family of cyclic lipopeptides reported to exhibit antifungal activity. We synthesized a series of 18 burkholdine analogues in good yield by conventional Fmoc-SPPS followed by cyclization with DIPCI/HOBt in the solution phase. Although none of the synthesized peptides exhibited...

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Bibliographic Details
Main Authors: Hiroyuki Konno, Mio Sasaki, Hinata Sano, Keima Osawa, Kazuto Nosaka, Shigekazu Yano
Format: Article
Language:English
Published: MDPI AG 2022-02-01
Series:Molecules
Subjects:
antifungal activity
cyclic octalipopeptide
burkholdine
potentiation effect
Online Access:https://www.mdpi.com/1420-3049/27/4/1191
Description
Summary:The burkholdines are a family of cyclic lipopeptides reported to exhibit antifungal activity. We synthesized a series of 18 burkholdine analogues in good yield by conventional Fmoc-SPPS followed by cyclization with DIPCI/HOBt in the solution phase. Although none of the synthesized peptides exhibited antifungal activity, several did potentiate the antibiotic effect of the antibiotic G418, including the Thr-bearing Bk analogue (<b>4b</b>) and the tartaramide-bearing Bk analogue (<b>5b</b>). This work exemplifies the potential of burkholdine analogues as potentiating agents.
ISSN:1420-3049

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