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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
The Hydrophobicity and Antifungal Potentiation of Burkholdine Analogues
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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