芳基 1,4-二氮杂烷类化合物作为强效和选择性的 CB2 激动剂：优化类药性和非靶标参数。
Aryl 1,4-diazepane compounds as potent and selective CB2 agonists: optimization of drug-like properties and target independent parameters.
机构信息
Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA.
出版信息
Bioorg Med Chem Lett. 2011 Jul 15;21(14):4276-80. doi: 10.1016/j.bmcl.2011.05.068. Epub 2011 May 27.
A high throughput screening campaign identified aryl 1,4-diazepane compounds as potent and selective cannabinoid receptor 2 agonists as compared to cannabinoid receptor 1. This class of compounds suffered from poor drug-like parameters as well as low microsomal stability and poor solubility. Structure-activity relationships are described with a focus on improving the drug-like parameters resulting in compounds with improved solubility and permeability.
高通量筛选活动发现，与大麻素受体 1 相比，芳基 1,4-二氮杂烷类化合物是一种有效的、选择性的大麻素受体 2 激动剂。该类化合物具有较差的类药性参数以及较差的微粒体稳定性和低溶解度。本文描述了这些化合物的构效关系，重点是改善药物样参数，从而提高化合物的溶解度和渗透性。
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