期刊
TETRAHEDRON LETTERS
卷 56, 期 27, 页码 4119-4123出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2015.05.035
关键词
1,3-Dipolar cycloaddition; 2-Isoxazoline; Fragment library; 3D-fragments; sp(3)-rich fragments
资金
- Agence Universitaire de la Francophonie (AUF)
- ANR [ANR-13-JSV5-0010-01]
- Inserm
- Universite Lille Nord de France
- Institut Pasteur de Lille
- EU
- Region Nord-Pas de Calais
- PRIM, Pole de Recherche Interdisciplinaire du Medicament
- Agence Nationale de la Recherche (ANR) [ANR-13-JSV5-0010] Funding Source: Agence Nationale de la Recherche (ANR)
The design of new sp(3) and spiro-enriched fragments has been achieved from 1,3-dipolar cycloaddition between alkenes and chloro-oximes. The selection of reagents was performed to afford a panel of 2-isoxazoline-containing fragments that show desirable three dimensional (3D) characteristics to allow the probing of biologically-relevant chemical space. Principal moments of inertia (PMI) were calculated to evaluate the 3D diversity. The resulting 3D fragments with suitable physicochemical properties, especially a good solubility, will be used to improve the hit rate of our fragment-based screening. (C) 2015 Elsevier Ltd. All rights reserved.
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