Novel echinocandin antifungals. Part 2: Optimization of the side chain of the natural product FR901379. Discovery of micafungin

Bioorganic & Medicinal Chemistry Letters
Masaki TomishimaFumiaki Ikeda

Abstract

Further optimization of the potent antifungal activity of side chain analogs of the natural product FR901379 led to the discovery of compound 8 with an excellent, well-balanced profile. Potent compounds with reduced hemolytic potential were designed based upon a disruption of the linearity of the terphenyl lipophilic side chain. The optimized compound (8, FK463, micafungin) displayed the best balance and was selected as the clinical candidate.

Citations

Jan 10, 2009·The Journal of Antibiotics·Seiji Hashimoto
Dec 2, 2010·The Journal of Antibiotics·Satoshi UedaSeiji Hashimoto
Jul 15, 2011·Journal of Bioscience and Bioengineering·Satoshi UedaSeiji Hashimoto
Mar 19, 2011·Chemistry, an Asian Journal·Akihiro GotoSusumu Saito
Oct 22, 2013·Natural Product Reports·Armin Bauer, Mark Brönstrup

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