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

Elizabeth M. Smith,Steve Sorota,Hyunjin M. Kim,Brian A. McKittrick,Terry Nechuta,Chad Bennett,Chad E. 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

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

2010

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.

Keywords:

Organic chemistry
Piperidine
Calcium channel
Potency
T-type calcium channel
Calcium channel blocker
Biochemistry
Chemistry
Stereochemistry
Neuropathic pain
Selectivity
Chemical synthesis
Lactam
Bicyclic molecule

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