Spock, Matthew; Carter, Trever R.; Bollinger, Katrina A.; Han, Changho; Baker, Logan A.; Rodriguez, Alice L.; Peng, Li; Dickerson, Jonathan W.; Qi, Aidong; Rook, Jerri M.; O’Neill, Jordan C.; Watson, Katherine J.; Chang, Sichen; Bridges, Thomas M.; Engers, Julie L.; Engers, Darren W.; Niswender, Colleen M.; Conn, P. Jeffrey; Lindsley, Craig W.; Bender, Aaron M. published the artcile< Discovery of VU6028418: A Highly Selective and Orally Bioavailable M4 Muscarinic Acetylcholine Receptor Antagonist>, Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine, the main research area is preparation oral mAChR4 antagonist dystonia movement disorder.
Herein, we report the SAR leading to the discovery of VU6028418, a potent M4 mAChR antagonist with high subtype-selectivity and attractive DMPK properties in vitro and in vivo across multiple species. VU6028418 was subsequently evaluated as a preclin. candidate for the treatment of dystonia and other movement disorders. During the characterization of VU6028418, a novel use of deuterium incorporation as a means to modulate CYP inhibition was also discovered.
ACS Medicinal Chemistry Letters published new progress about Canis familiaris. 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine.