Abstract
Benzofuran N-myristoyltransferase inhibitors showing antifungal activity in vivo were obtained by modifying a screening hit that showed only marginal antifungal activity in vitro. The modification design was based on the analysis of X-ray crystal structures of Candida albicans N-myristoyltransferase complexes with benzofurans. The modification was mainly guided by enzyme inhibitory activity, antifungal activity in vitro, quasi in viva assay and pharmacokinetic properties. The biological activities of one of the most promising benzofuran inhibitors. RO-09-4879, are described in detail. The multidimensional optimization and potential of benzofuran innibitors as antifungal drugs are also discussed.
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