T 型钙通道阻滞剂：螺哌啶氮杂环丁烷和氮杂环丁酮的优化、设计和合成。
T-type calcium channel blockers: spiro-piperidine azetidines and azetidinones-optimization, design and synthesis.
机构信息
Department of Medicinal Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2010 Aug 1;20(15):4602-6. doi: 10.1016/j.bmcl.2010.06.012. Epub 2010 Jun 8.
PMID:20580233
Abstract
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.
摘要
一系列螺环氮杂环丁烷和氮杂环丁酮类化合物已被评估为新型 T 型钙通道（Ca(V)3.2）阻滞剂，该通道是治疗炎症性和神经性疼痛的新治疗靶点。本文将介绍先导化合物的效力、选择性和 DMPK 性质的确认和优化。
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