基于氨基吡啶甲酰胺的抑制剂：结构-活性关系。
Aminopyridinecarboxamide-based inhibitors: Structure-activity relationship.
机构信息
Department of Medicinal Chemistry, Pfizer Inc, 700 Chesterfield Parkway West, St Louis, MO 63017, United States.
出版信息
Bioorg Med Chem. 2010 Jan 1;18(1):403-14. doi: 10.1016/j.bmc.2009.10.040. Epub 2009 Oct 27.
PMID:19914076
Abstract
Series of aminopyridinecarboxamide-based inhibitors were synthesized and tested against human recombinant IKK-2 and in IL-1beta stimulated synovial fibroblasts. The 2-amino-5-chloropyridine-4-carboxamides were identified as the most potent inhibitors with improved cellular activity.
摘要
一系列基于氨基吡啶甲酰胺的抑制剂被合成并针对人重组 IKK-2 和白细胞介素-1β刺激的滑膜成纤维细胞进行了测试。2-氨基-5-氯吡啶-4-甲酰胺被鉴定为最有效的抑制剂，具有改善的细胞活性。
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