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

A series of spiro-azetidines and azetidinones has been evaluated as novel blockers of the T-type calcium channel (CaV3.2) 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 proper...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-08, Vol.20 (15), p.4602-4606
Hauptverfasser:	Smith, Elizabeth M., Sorota, Steve, Kim, Hyunjin M., McKittrick, Brian A., Nechuta, Terry L., Bennett, Chad, Knutson, Chad, Burnett, Duane A., Kieselgof, Jane, Tan, Zheng, Rindgen, Diane, Bridal, Terry, Zhou, Xiaoping, Jia, Yu-Ping, Dong, Zoe, Mullins, Debbie, Zhang, Xiaoping, Priestley, Tony, Correll, Craig C., Tulshian, Deen, Czarniecki, Michael, Greenlee, William J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Azetidines - chemical synthesis Azetidines - chemistry Azetidines - therapeutic use Biological and medical sciences Calcium Channel Blockers - chemical synthesis Calcium Channel Blockers - chemistry Calcium Channel Blockers - therapeutic use Calcium Channels, T-Type - chemistry Calcium Channels, T-Type - metabolism Drug Design Humans Medical sciences Miscellaneous Neuropathic pain Pain - drug therapy Pharmacology. Drug treatments Piperidines - chemistry Protein Binding Rats Spiro Compounds - chemistry Spiro-azetidines Spiro-azetidinones Structure-Activity Relationship T-type calcium channel (CaV3.2)
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Zusammenfassung:	A series of spiro-azetidines and azetidinones has been evaluated as novel blockers of the T-type calcium channel (CaV3.2) 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.06.012