title: Novel hypoglycemic dihydropyridones serendipitously discovered from O- versus C-alkylation in the synthesis of VMAT2 antagonists.
abstract: Vesicular monoamine transporter type 2 (VMAT2) is a newly emerging target for both diagnostic and therapeutic applications in diabetes mellitus. In pursuit of novel VMAT2 antagonists, we identified a potent hypoglycemic agent with a novel dihydropyridone scaffold. Several analogs were designed and synthesized. A preliminary structure activity relationship (SAR) showed that the dihydropyridone scaffold is required for the activity.
authors.affiliation: Department of Medicine, Columbia University Medical Center, New York, NY 10032, USA.
authors.forename: Yuli
authors.initials: Y
authors.lastname: Xie
authors.forename: Anthony
authors.initials: A
authors.lastname: Raffo
authors.forename: Masanori
authors.initials: M
authors.lastname: Ichise
authors.forename: Shixian
authors.initials: S
authors.lastname: Deng
authors.forename: Paul E
authors.initials: PE
authors.lastname: Harris
authors.forename: Donald W
authors.initials: DW
authors.lastname: Landry