Discovery of novel potent imidazo[1, 2-b]pyridazine PDE10a inhibitors. Issue 17 (1st September 2016)

• Record Type: Journal Article
• Authors: Meegalla, Sanath K.; Huang, Hui; Illig, Carl R.; Parks, Daniel J.; Chen, Jinsheng; Lee, Yu-Kai; Wilson, Kenneth J.; Patel, Sharmila K.; Cheung, Wing S.; Lu, Tianbao; Kirchner, Thomas; Askari, Hossein B.; Geisler, John; Patch, Raymond J.; Gibbs, Alan C.; Rady, Brian; Connelly, Margery; Player, Mark R.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 17(2016)
• Page Start: 4216
• Page End: 4222
• Publication Date: 2016-09-01
• Subjects: PDE10a inhibitor -- Insulin secretagogues -- Type 2 diabetes -- GPCR -- GSIS -- Brain penetration; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.07.054
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Design and optimization of a novel series of imidazo[1, 2-b]pyridazine PDE10a inhibitors are described. Compound31 displays excellent pharmacokinetic properties and was also evaluated as an insulin secretagogue in vitro and in vivo.