The Hydrophobicity and Antifungal Potentiation of Burkholdine Analogues
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Updated: Oct 2, 2025

Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds
Published on: February 14, 2018
Hiroyuki Konno1, Mio Sasaki1, Hinata Sano1
1Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa 992-8510, Japan.
Abstract:
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 (4b) and the tartaramide-bearing Bk analogue (5b). This work exemplifies the potential of burkholdine analogues as potentiating agents.
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