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首页> 外文期刊>Chemistry: A European journal >1,3,5-Triazepan-2,6-diones as Structurally Diverse and Conformationally Constrained Dipeptide Mimetics:Identification of Malaria Liver Stage Inhibitors from a Small Pilot Library
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1,3,5-Triazepan-2,6-diones as Structurally Diverse and Conformationally Constrained Dipeptide Mimetics:Identification of Malaria Liver Stage Inhibitors from a Small Pilot Library

机译：1,3,5-Triazepan-2,6-diones作为结构多样且构象受约束的二肽模拟物：从一个小型试验库中鉴定出疟疾肝阶段抑制剂

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摘要

The development of the 1,3,5-triazepan-2,6-dione system as a novel,conformationally restricted,and readily accessible class of dipeptidomi-metics is reported.The synthesis of the densely functionalized 1,3,5-triazepan-2,6-dione skeleton was achieved in only four steps from a variety of simple linear dipeptide precursors.To extend the practical value of 1,3,5-triazepane-2,6-diones,a general polymer-assisted solution-phase synthesis approach amenable to library production in a multiparallel format was developed.The conformational preferences of the 1,3,5-triazepan-2,6-dione skeleton were investigated in detail by NMR spectros-copy and X-ray diffraction.The ring exhibits a characteristic folded conformation which was compared to that of related dipeptide-derived scaffolds including the more planar 2,5-diketopi-perazine (DKP).Molecular and structural diversity was increased further through post-cyclization appending operations at urea nitrogens.Preliminary biological screens of a small collection of 1,3,5-triazepan-2,6-diones revealed inhibitors of the underexplored malaria liver stage and suggest strong potential for this dipeptide-derived scaffold to interfere with and to modulate biological pathways.
机译：据报道，1,3,5-triazepan-2,6-dione系统是一种新型的，构象受限的，易于获得的二肽模拟物类。据报道，稠密官能化的1,3,5-triazepan-从各种简单的线性二肽前体中仅需四个步骤即可获得2,6-二酮骨架。为扩展1,3,5-三氮杂环庚烷-2,6-二酮的实用价值，采用常规的聚合物辅助溶液相合成方法开发了一种适用于多平行形式的文库生产的方法。通过NMR光谱和X射线衍射详细研究了1,3,5-triazepan-2,6-dione骨架的构象偏好。与相关的二肽衍生的支架（包括更平坦的2,5-二酮-哌嗪（DKP））相比，具有独特的折叠构象。通过在尿素氮上进行环化后附加操作，分子和结构的多样性进一步增加。一个小col 1,3,5-triazepan-2,6-diones的选择揭示了未充分开发的疟疾肝阶段的抑制剂，并表明这种二肽衍生的支架具有强大的潜力来干扰和调节生物学途径。

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