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Structure activity relationship study of burkholdine analogues toward simple antifungal agents.
Konno, Hiroyuki; Abumi, Kanako; Sasaki, Yasuhiro; Yano, Shigekazu; Nosaka, Kazuto.
Afiliación
  • Konno H; Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, 4-3-16 Jonan, Yonezawa, Yamagata 992-8510, Japan. Electronic address: konno@yz.yamagata-u.ac.jp.
  • Abumi K; Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, 4-3-16 Jonan, Yonezawa, Yamagata 992-8510, Japan.
  • Sasaki Y; Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, 4-3-16 Jonan, Yonezawa, Yamagata 992-8510, Japan.
  • Yano S; Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, 4-3-16 Jonan, Yonezawa, Yamagata 992-8510, Japan.
  • Nosaka K; School of Pharmacy and Pharmaceutical Sciences, Mukogawa Women's University, 9-11-68 Koshien, Nishinomiya, Hyogo 663-8179, Japan.
Bioorg Med Chem Lett ; 25(16): 3199-202, 2015 Aug 15.
Article en En | MEDLINE | ID: mdl-26077490
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.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Péptidos Cíclicos / Lipopéptidos / Antifúngicos Idioma: En Año: 2015 Tipo del documento: Article
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Péptidos Cíclicos / Lipopéptidos / Antifúngicos Idioma: En Año: 2015 Tipo del documento: Article