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

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)

Abstract

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.

Original languageEnglish
JournalOrganic Letters
DOIs
Publication statusPublished - 2019 Jan 1

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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