合成及结构-活性关系（SAR）研究 4-氮杂苯并恶唑类似物作为 H3 拮抗剂。
Synthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H3 antagonists.
机构信息
Chemical Research Department, Department of Chemical Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2012 Mar 1;22(5):2075-8. doi: 10.1016/j.bmcl.2012.01.020. Epub 2012 Jan 24.
PMID:22326166
Abstract
The synthesis and SAR of a novel series of 4-azabenzoxazole histamine H(3) antagonists is described. Introduction of substituted phenyl, pyridyl and fused heterocyclic groups to the 6-position of the 4-azabenzoxazole core gave a series of compounds with good H(3) antagonist activity in both ex vivo and in vivo assays.
摘要
描述了一系列新型 4-氮杂苯并恶唑组胺 H(3)拮抗剂的合成和 SAR。在 4-氮杂苯并恶唑核心的 6 位引入取代的苯基、吡啶基和稠合杂环基团，得到了一系列在离体和体内试验中均具有良好 H(3)拮抗活性的化合物。
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