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- W2079201901 endingPage "4478" @default.
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- W2079201901 abstract "The C-4 side chain modification of lead compound 1 has resulted in the identification of a potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitor RO-09-4609, which exhibits antifungal activity against C. albicans in vitro. Further modification of its C-2 substituent has led to the discovery of RO-09-4879, which exhibits antifungal activity in vivo. The drug design is based on X-ray crystal analysis of a CaNmt complex with benzofuran derivative 4a. The optimization incorporates various biological investigations including a quasi in vivo assay and pharmacokinetic study. The computer aided drug design, synthesis, structure-activity relationships, and biological properties of RO-09-4879 are described in detail." @default.
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- W2079201901 date "2003-10-01" @default.
- W2079201901 modified "2023-09-25" @default.
- W2079201901 title "Synthesis and biological activities of benzofuran antifungal agents targeting fungal N-myristoyltransferase" @default.
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- W2079201901 doi "https://doi.org/10.1016/s0968-0896(03)00429-2" @default.
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