Kozupeptins, Antimalarial Agents Produced by Paracamarosporium Species: Isolation, Structural Elucidation, Total Synthesis, and Bioactivity

Yumi Hayashi, Wataru Fukasawa, Tomoyasu Hirose, Masato Iwatsuki, Rei Hokari, Aki Ishiyama, Masahiro Kanaida, Kenichi Nonaka, Akira Take, Kazuhiko Otoguro, Satoshi Omura, Kazuro Shiomi*, Toshiaki Sunazuka

*この研究の対応する著者

研究成果査読

6 被引用数 (Scopus)

抄録

Kozupeptins A and B, novel antimalarial lipopeptides, were isolated from the culture broths of Paracamarosporium sp. FKI-7019. They exhibited potent antimalarial activity against chloroquine-sensitive and -resistant Plasmodium falciparum strains in vitro. The structural elucidation was accomplished by a combination of spectroscopic analyses and chemical approaches including a total synthesis of kozupeptin A. Synthetic kozupeptin A demonstrated a therapeutic effect in vivo, and an intermediate exhibited much higher antimalarial activity than kozupeptin A.

本文言語English
ジャーナルOrganic Letters
DOI
出版ステータスPublished - 2019 1 1

ASJC Scopus subject areas

  • 生化学
  • 物理化学および理論化学
  • 有機化学

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