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

Research output: Contribution to journalArticle

3 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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    Hayashi, Y., Fukasawa, W., Hirose, T., Iwatsuki, M., Hokari, R., Ishiyama, A., Kanaida, M., Nonaka, K., Take, A., Otoguro, K., Omura, S., Shiomi, K., & Sunazuka, T. (2019). Kozupeptins, Antimalarial Agents Produced by Paracamarosporium Species: Isolation, Structural Elucidation, Total Synthesis, and Bioactivity. Organic Letters. https://doi.org/10.1021/acs.orglett.9b00483