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Updated: May 21, 2026

Synthesis of Information-bearing Peptoids and their Sequence-directed Dynamic Covalent Self-assembly
Published on: February 6, 2020
Synthesis of pacidamycin analogues via an Ugi-multicomponent reaction
Kazuya Okamoto1, Masahiro Sakagami, Fei Feng
1Shionogi Innovation Center for Drug Discovery, Shionogi & Co., Ltd, Kita-21, Nishi-11, Kita-ku, Sapporo 001-0021, Japan.
Abstract:
The second-generation synthesis of 3'-hydroxypacidamycin D (2) has been accomplished via an Ugi-four component reaction at a late stage of the synthesis. This approach provided ready access to a range of analogues including diastereomers of the diaminobutylic acid residue and hybrid-type analogues of mureidomycins. Biological evaluations of these analogues indicated that the stereochemistry at the diaminobutylic acid residue has a crucial impact on both the MraY biochemical inhibition and whole-cell antibacterial activity.
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