Structure activity relationship study of burkholdine analogues toward simple antifungal agents.

Abstract:

:Cyclic and linear lipopeptides, burkholdine analogues, were synthesized by conventional Fmoc-SPPS and cyclisation with DIPC/HOBt in the solution phase. Synthesized peptides were evaluated for antifungal activities with MIC values against Saccharomyces cerevisiae and Aspergillus oryzae. As a result, the stereochemistry of the amino acid residues and sequences of burkholdine analogues exerted a significant influence on antifungal activities. In addition, we found a linear burkholdine analogue with moderate antifungal activities.

journal_name

Bioorg Med Chem Lett

authors

Konno H,Abumi K,Sasaki Y,Yano S,Nosaka K

doi

10.1016/j.bmcl.2015.05.088

subject

Has Abstract

pub_date

2015-08-15 00:00:00

pages

3199-202

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)00571-5

journal_volume

25

pub_type

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