基于咪唑并[4,5-d]噻唑并[5,4-b]吡啶的 IKK2 抑制剂：合成、SAR、药代动力学/药效学研究及在类风湿关节炎临床前模型中的活性。
Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.
机构信息
Bristol-Myers Squibb, Research and Development, Princeton, NJ 08543-4000, USA.
出版信息
Bioorg Med Chem Lett. 2011 Jan 1;21(1):383-6. doi: 10.1016/j.bmcl.2010.10.133. Epub 2010 Oct 31.
PMID:21087862
Abstract
The synthesis, structure-activity relationships (SAR) and biological evaluation of thiazole based tricyclic inhibitors of IKK2 are described. Compound 9 was determined to be orally efficacious in a murine model of rheumatoid arthritis.
摘要
本文描述了基于噻唑的三环 IKK2 抑制剂的合成、构效关系（SAR）和生物评价。化合物 9 在类风湿性关节炎的小鼠模型中被确定具有口服疗效。
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