具有 2,2-二甲基-3-苯基-N-(噻唑或噻二唑-2-基)丙酰胺核心的杂环糖皮质激素受体调节剂。
Heterocyclic glucocorticoid receptor modulators with a 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core.
机构信息
Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543-4000, United States.
出版信息
Bioorg Med Chem Lett. 2013 Oct 15;23(20):5571-4. doi: 10.1016/j.bmcl.2013.08.049. Epub 2013 Aug 16.
PMID:24011644
Abstract
A series of heterocyclic glucocorticoid receptor (GR) modulators with 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core are described. Structure-activity relationships suggest a combination of H-bond acceptor and a 4-fluorophenyl moiety as being important structural components contributing to the glucocorticoid receptor binding and functional activity for this series of GR modulators.
摘要
描述了一系列具有 2,2-二甲基-3-苯基-N-(噻唑或噻二唑-2-基)丙酰胺核心的杂环糖皮质激素受体 (GR) 调节剂。构效关系表明，氢键受体和 4-氟苯基部分的结合是这一系列 GR 调节剂与糖皮质激素受体结合和功能活性的重要结构组成部分。
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