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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 2.

Modification of the C-2 position of a benzofuran derivative 6 (RO-09-4609), an N-myristoyltransferase ( Nmt) inhibitor, has led us to discover antifungal agents that are active in a murine systemic candidiasis model. The drug design is based on the analysis of a crystal structure of a Candida Nmt complex with 2. The optimization has been guided by various biological evaluations including a quasi in vivo assay and pharmacokinetic analysis.[1]

References

  1. Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 2. Ebiike, H., Masubuchi, M., Liu, P., Kawasaki, K., Morikami, K., Sogabe, S., Hayase, M., Fujii, T., Sakata, K., Shindoh, H., Shiratori, Y., Aoki, Y., Ohtsuka, T., Shimma, N. Bioorg. Med. Chem. Lett. (2002) [Pubmed]
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