521917-51-1Relevant articles and documents
Azologization and repurposing of a hetero-stilbene-based kinase inhibitor: Towards the design of photoswitchable sirtuin inhibitors
Grathwol, Christoph W.,W?ssner, Nathalie,Swyter, S?ren,Smith, Adam C.,Tapavicza, Enrico,Hofstetter, Robert K.,Bodtke, Anja,Jung, Manfred,Link, Andreas
, p. 2170 - 2183 (2019/09/30)
The use of light as an external trigger to change ligand shape and as a result its bioactivity, allows the probing of pharmacologically relevant systems with spatiotemporal resolution. A hetero-stilbene lead resulting from the screening of a compound that was originally designed as kinase inhibitor served as a starting point for the design of photoswitchable sirtuin inhibitors. Because the original stilbenoid structure exerted unfavourable photochemical characteristics it was remodelled to its heteroarylic diazeno analogue. By this intramolecular azologization, the shape of the molecule was left unaltered, whereas the photoswitching ability was improved. As anticipated, the highly analogous compound showed similar activity in its thermodynamically stable stretched-out (E)-form. Irradiation of this isomer triggers isomerisation to the long-lived (Z)-configuration with a bent geometry causing a considerably shorter end‐to‐end distance. The resulting affinity shifts are intended to enable real‐time photomodulation of sirtuins in vitro.
2-Styryl-pyridines and 2-(3,4-Dihydro-naphthalen-2-yl)-pyridines as potent NR1/2B subtype selective NMDA receptor antagonists
Buettelmann, Bernd,Alanine, Alexander,Bourson, Anne,Gill, Ramanjit,Heitz, Marie-Paule,Mutel, Vincent,Pinard, Emmanuel,Trube, Gerhard,Wyler, Rene
, p. 630 - 633 (2007/10/03)
A series of 2-styryl-pyridines and 2-(3,4-dihydro-naphthalen-2-yl)- pyridines was prepared and evaluated as NR1/2B subtype selective NMDA receptor antagonists. The SAR developed in this series resulted in the discovery of high affinity antagonists that are selective (vs. α1 and M 1 receptors) and are active in vivo.
Substituted imidazol-pyridazine derivatives
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Page 20, (2010/02/05)
The present invention relates to compounds of formula wherein A is an unsubstituted or substituted cyclic group; and R is hydrogen or lower alkyl; or a pharmaceutically acceptable acid addition salt thereof. These compounds are NMDA NR-2B receptor subtype specific blockers and are useful in the treatment of neurodegeneration, depression and pain.