Actinoallolides A–E, New Anti-trypanosomal Macrolides, Produced by an Endophytic Actinomycete, <i>Actinoallomurus fulvus</i> MK10-036

Yuki Inahashi, Masato Iwatsuki, Aki Ishiyama, Atsuko Matsumoto, Tomoyasu Hirose, Jun Oshita, Toshiaki Sunazuka, Watanalai Panbangred, Yōko Takahashi, Marcel Kaiser,

Organic Letters · 2015 · 63 citations · 7 references

Concepts

Abstract

Five new anti-trypanosomal macrolides, actinoallolides A-E (1-5), were discovered from the cultured broth of Actinoallomurus fulvus MK10-036. The structures of the actinoallolides, including absolute stereochemistry, were elucidated by a combination of spectroscopic analyses and a series of chemical derivatization studies. Actinoallolide A showed the most potent and selective in vitro anti-trypanosomal activity without cytotoxicity. A new class of promising lead compounds was identified for the development of drugs for both sleeping sickness and Chagas disease.

References

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