T-type calcium channel blockers: spiro-piperidine azetidines and azetidinones—optimization, design and synthesis
2010; Elsevier BV; Volume: 20; Issue: 15 Linguagem: Inglês
10.1016/j.bmcl.2010.06.012
ISSN1464-3405
AutoresElizabeth M. Smith, Steve Sorota, Hyunjin M. Kim, Brian A. McKittrick, Terry L. Nechuta, Chad Bennett, Chad Knutson, Duane A. Burnett, Jane Kieselgof, Zheng Lin Tan, Diane Rindgen, Terry Bridal, Zhou Xiao-ping, Yuping Jia, Zoe Dong, Debbie Mullins, Xiaoping Zhang, Tony Priestley, Craig C. Correll, Deen Tulshian, Michael Czarniecki, William J. Greenlee,
Tópico(s)Synthesis of β-Lactam Compounds
ResumoA 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.
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