1,4-二氮杂烷类化合物作为有效且选择性的 CB2 激动剂：代谢稳定性的优化。
1,4-Diazepane compounds as potent and selective CB2 agonists: optimization of metabolic stability.
机构信息
Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc, 900 Ridgebury Road, Ridgefield, CT 06877, USA.
出版信息
Bioorg Med Chem Lett. 2011 Apr 1;21(7):2011-6. doi: 10.1016/j.bmcl.2011.02.017. Epub 2011 Feb 25.
PMID:21354795
Abstract
A high-throughput screening campaign has identified 1,4-diazepane compounds which are potent Cannabinoid receptor 2 agonists with excellent selectivity against the Cannabinoid receptor 1. This class of compounds suffered from low metabolic stability. Following various strategies, compounds with a good stability in liver microsomes and rat PK profile have been identified.
摘要
高通量筛选活动已经确定了 1,4-二氮杂环庚烷类化合物，它们是有效的大麻素受体 2 激动剂，对大麻素受体 1 具有优异的选择性。这一类化合物的代谢稳定性较低。通过各种策略，已经确定了在肝微粒体和大鼠 PK 特征中具有良好稳定性的化合物。
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