D-Proline-based peptidomimetic inhibitors of anthrax lethal factor

C Calugi, A Trabocchi, C Lalli, A Guarna

文献索引：Calugi, Chiara; Trabocchi, Andrea; Lalli, Claudia; Guarna, Antonio European Journal of Medicinal Chemistry, 2012 , vol. 56, p. 96 - 107

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被引用次数: 3

摘要

In this work we reported the generation of d-proline-derived hydroxamic acids as inhibitors of anthrax lethal factor (LF), taking advantage of a pyrrolidine ring as the central scaffold and a hydroxamate group as the Zn2+ chelating agent. The introduction of two hydrophobic groups addressing the S1′ subsite and a long substrate-binding groove was conceived by overlapping the bioactive conformations of two reported LF inhibitors. Micromolar affinity ...