131-65-7Relevant academic research and scientific papers
Diversification of edaravone via palladium-catalyzed hydrazine cross-coupling: Applications against protein misfolding and oligomerization of beta-amyloid
Maclean, Mark A.,Diez-Cecilia, Elena,Lavery, Christopher B.,Reed, Mark A.,Wang, Yanfei,Weaver, Donald F.,Stradiotto, Mark
, p. 100 - 104 (2015/12/18)
N-Aryl derivatives of edaravone were identified as potentially effective small molecule inhibitors of tau and beta-amyloid aggregation in the context of developing disease-modifying therapeutics for Alzheimer's disease (AD). Palladium-catalyzed hydrazine monoarylation protocols were then employed as an expedient means of preparing a focused library of 21 edaravone derivatives featuring varied N-aryl substitution, thereby enabling structure-activity relationship (SAR) studies. On the basis of data obtained from two functional biochemical assays examining the effect of edaravone derivatives on both fibril and oligomer formation, it was determined that derivatives featuring an N-biaryl motif were four-fold more potent than edaravone.
P2Y1 receptor antagonists as novel antithrombotic agents
Pfefferkorn, Jeffrey A.,Choi, Chulho,Winters, Thomas,Kennedy, Robert,Chi, Liguo,Perrin, Lisa A.,Lu, Gina,Ping, Yun-Wen,McClanahan, Tom,Schroeder, Richard,Leininger, Michael T.,Geyer, Andrew,Schefzick, Sabine,Atherton, James
body text, p. 3338 - 3343 (2009/04/06)
The P2Y1 and P2Y12 purinergic receptors are responsible for mediating adenosine diphosphate (ADP) dependent platelet aggregation. Evidence from P2Y1 knockout studies as well as from nucleotide-based small molecule P2Y1 antagonists has suggested that the antagonism of this receptor may offer a novel and effective method for the treatment of thrombotic disorders. Herein, we report the identification and optimization of a series of non-nucleotide P2Y1 antagonists that are potent and orally bioavailable.
