842954-77-2Relevant academic research and scientific papers
Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery
Tran, Ngoc Chau,Dhondt, Heleen,Flipo, Marion,Deprez, Benoit,Willand, Nicolas
supporting information, p. 4119 - 4123 (2015/08/03)
Abstract The design of new sp3 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.
Synthesis and evaluation of 4,5-dihydro-5-methylisoxazolin-5-carboxamide derivatives as VLA-4 antagonists
Soni, Ajay,Rehman, Abdul,Naik, Keshav,Dastidar, Sunanda,Alam,Ray, Abhijit,Chaira, Tridib,Shah, Vanya,Palle, Venkata P.,Cliffe, Ian A.,Sattigeri, Viswajanani J.
, p. 1482 - 1485 (2013/03/14)
A novel set of compounds containing a 4,5-dihydro-5-methylisoxazoline have been successfully designed as VLA-4 receptor antagonists. Compound (14p) had a high receptor binding affinity of 4 nM and also found to be metabolically stable in vitro.
HETEROCYCLIC DERIVATIVES AS CELL ADHESION INHIBITORS
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Page/Page column 33-34, (2008/06/13)
The present invention relates to certain heterocyclic derivatives of formula (I) , in particular isoxazoline and isothiazoline derivatives as cell adhesion inhibitors. The compounds of this invention can be useful, for inhibition and prevention of cell ad
CASPASE INHIBITORS CONTAINING ISOXAZOLINE RING
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Page/Page column 22-23, (2008/06/13)
The present invention relates to an isoxazoline derivative as an inhibitor against various caspases, a process for preparing the same, and a therapeutic composition for preventing inflammation and apoptosis comprising the same
