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 (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. (C) 2010 Elsevier Ltd. All rights reserved.