1.
ACS Med Chem Lett
; 12(8): 1342-1349, 2021 Aug 12.
Article
in English
| MEDLINE
| ID: mdl-34413964
ABSTRACT
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 preclinical 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.