期刊
TETRAHEDRON LETTERS
卷 57, 期 26, 页码 2888-2894出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2016.05.065
关键词
Fragment library; 3-D shape analysis; Spiranic center; Spirohydantoin; Microwave synthesis
资金
- Inserm
- Universite Lille Nord de France
- Institut Pasteur de Lille
- EU
- Region Nord-Pas de Calais
- PRIM Pole de Recherche Interdisciplinaire du Medicament
- ANR [ANR-13-JSV5-0010-01]
- Agence Nationale de la Recherche (ANR) [ANR-13-JSV5-0010] Funding Source: Agence Nationale de la Recherche (ANR)
Fragment-based drug design has been successfully applied to a large set of proteins, however in order to expand this concept to the most demanding targets, such as protein-protein interactions, it is required to enrich current fragment libraries with new and original 3D privileged fragments. Our goal was to develop a rapid microwave-assisted synthesis of 27 new privileged spirohydantoin fragments. Among them 24 compounds showed a high water solubility. These molecules were plotted according to the normalized principal moments of inertia of their minimized conformers, and most of the compounds were prone to occupy under-populated regions of the triangular plot. Finally we demonstrated that the hydantoin ring can be selectively N-monoalkylated providing the access to rapid functionalization for further elaboration. (C) 2016 Elsevier Ltd. All rights reserved.
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