生成 3,8-取代的 1,2,4-三唑并吡啶作为人 11β-羟甾脱氢酶 1 型（11β-HSD-1）的有效抑制剂。
Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1).
机构信息
Research and Development, Bristol-Myers Squibb, PO Box 5400, Princeton, NJ 08543, USA.
出版信息
Bioorg Med Chem Lett. 2011 Jul 15;21(14):4146-9. doi: 10.1016/j.bmcl.2011.05.101.
PMID:21689935
Abstract
A series of pyridyl amide/sulfonamide inhibitors of 11β-HSD-1 were modified to incorporate a novel 1,2,4-triazolopyridine scaffold. Optimization of substituents at the 3 and 8 position of the TZP core, with a special focus on enhancing metabolic stability, resulted in the identification of compound 38 as a potent and metabolically stable inhibitor of the enzyme.
摘要
一系列 11β-HSD-1 的吡啶酰胺/磺胺抑制剂被修饰以纳入新型 1,2,4-三唑并吡啶骨架。对 TZP 核心的 3 和 8 位取代基进行优化，特别关注增强代谢稳定性，导致鉴定出化合物 38 为该酶的有效且代谢稳定的抑制剂。
Zotero 插件