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

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...

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Published inOrganic letters Vol. 21; no. 7; pp. 2180 - 2184
Main Authors Hayashi, Yumi, Fukasawa, Wataru, Hirose, Tomoyasu, Iwatsuki, Masato, Hokari, Rei, Ishiyama, Aki, Kanaida, Masahiro, Nonaka, Kenichi, Také, Akira, Otoguro, Kazuhiko, O̅mura, Satoshi, Shiomi, Kazuro, Sunazuka, Toshiaki
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 05.04.2019
Amer Chemical Soc
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
REAGENT
IN-VITRO
PROTECTING GROUP
AMINO-ACIDS
SUPPORTS
PHASE PEPTIDE-SYNTHESIS
DRUG-RESISTANT STRAINS
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Summary: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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.9b00483