Spiro-piperidine azetidinones as potent TRPV1 antagonists

…, A Palani, R Aslanian, BA McKittrick, AT McPhail…

Index: Xiao, Dong; Palani, Anandan; Aslanian, Robert; McKittrick, Brian A.; McPhail, Andrew T.; Correll, Craig C.; Phelps, P. Tara; Anthes, John C.; Rindgen, Diane Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 3 p. 783 - 787

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Citation Number: 12

Abstract

A series of spiro-piperidine azetidinone were synthesized and evaluated as potential TRPV1 antagonists. An important issue of plasma stability was investigated and resolved. Further focused SAR study lead to the discovery of a potent antagonist with good oral pharmacokinetic profile in rat.