394653-39-5Relevant articles and documents
Synthesis and preliminary biological evaluation at the glycineB site of (+)- and (-)-3-oxetanylglycine, novel non-proteinogenic amino acids
Del Carmen Teran Moldes, Maria,Costantino, Gabriele,Marinozzi, Maura,Pellicciari, Roberto
, p. 609 - 613 (2001)
Two novel non-proteinogenic amino acids, (+)- and (-)-3-oxetanylglycine were synthesized and evaluated for their ability to diplace [3H]-glycine from the glycine site of the NMDA receptor complex. The lack of activity of these compounds at conc
Construction of a Shape-Diverse Fragment Set: Design, Synthesis and Screen against Aurora-A Kinase
Zhang, Rong,McIntyre, Patrick J.,Collins, Patrick M.,Foley, Daniel J.,Arter, Christopher,von Delft, Frank,Bayliss, Richard,Warriner, Stuart,Nelson, Adam
supporting information, p. 6831 - 6839 (2019/05/10)
Historically, chemists have explored chemical space in a highly uneven and unsystematic manner. As an example, the shape diversity of existing fragment sets does not generally reflect that of all theoretically possible fragments. To assess experimentally the added value of increased three dimensionality, a shape-diverse fragment set was designed and collated. The set was assembled by both using commercially available fragments and harnessing unified synthetic approaches to sp3-rich molecular scaffolds. The resulting set of 80 fragments was highly three-dimensional, and its shape diversity was significantly enriched by twenty synthesised fragments. The fragment set was screened by high-throughput protein crystallography against Aurora-A kinase, revealing four hits that targeted the binding site of allosteric regulators. In the longer term, it is envisaged that the fragment set could be screened against a range of functionally diverse proteins, allowing the added value of more shape-diverse screening collections to be more fully assessed.
FUSED MORPHOLINOPYRIMIDINES AND METHODS OF USE THEREOF
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Paragraph 1172, (2017/05/14)
The present disclosure relates to Fused Morpholinopyrimidines, pharmaceutical compositions comprising an effective amount of a Fused Morpholinopyrimidine and methods for using a Fused Morpholinopyrimidine in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of a Fused Morpholinopyrimidine.
