取代的咪唑并[1,2-a]吡啶作为β-折叠肽模拟物。
Substituted imidazo[1,2-a]pyridines as β-strand peptidomimetics.
机构信息
Drug Discovery Department, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida 33612, United States.
出版信息
Org Lett. 2012 Dec 21;14(24):6162-5. doi: 10.1021/ol302850n. Epub 2012 Dec 4.
Abstract
New conformationally extended dipeptide surrogates based on an imidazo[1,2-a]pyridine scaffold are described. Efficient synthesis and incorporation into host peptides affords structures with native side-chain functionality and hydrogen bonding elements on one face of the backbone. Structural analysis by NMR suggests that model peptidomimetics adopt a β-strand-like conformation in solution.
摘要
本文描述了基于咪唑并[1,2-a]吡啶骨架的新型构象扩展二肽类似物。这些类似物通过高效合成并整合到宿主肽中，得到了具有天然侧链功能和骨架一侧氢键元件的结构。通过 NMR 的结构分析表明，模型拟肽在溶液中采取β-折叠样构象。
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