T-type calcium channel blockers: spiro-piperidine azetidines and azetidinones—optimization, design and synthesis

✍ Scribed by Elizabeth M. Smith; Steve Sorota; Hyunjin M. Kim; Brian A. McKittrick; Terry L. Nechuta; Chad Bennett; Chad Knutson; Duane A. Burnett; Jane Kieselgof; Zheng Tan; Diane Rindgen; Terry Bridal; Xiaoping Zhou; Yu-Ping Jia; Zoe Dong; Debbie Mullins; Xiaoping Zhang; Tony Priestley; Craig C. Correll; Deen Tulshian; Michael Czarniecki; William J. Greenlee

• Book ID: 104004496
• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 602 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.06.012

✦ Synopsis

A series of spiro-azetidines and azetidinones has been evaluated as novel blockers of the T-type calcium channel (Ca(V)3.2) which is a new therapeutic target for the potential treatment of both inflammatory and neuropathic pain. Confirmation and optimization of the potency, selectivity and DMPK properties of leads will be described.