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

M Tomishima, H Ohki, A Yamada, K Maki…

文献索引：Tomishima, Masaki; Ohki, Hidenori; Yamada, Akira; Maki, Katsuyuki; Ikeda, Fumiaki Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 9 p. 2886 - 2890

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被引用次数: 25

摘要

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.