Synthesis of 4H-1,4-oxazines as transthyretin amyloid fibril inhibitors

被引：7

作者：

Li, Weipeng ^{[1
]}

Duan, Xiaowei ^{[1
]}

Yan, Hong ^{[1
]}

Xin, Hongxing ^{[1
]}

机构：

[1] Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2013年 / 11卷 / 27期

关键词：

KINETIC STABILIZATION; NATIVE-STATE; BIOLOGICAL EVALUATION; OLIGOMERIC PROTEIN; DISEASE; DESIGN; AMYLOIDOGENESIS; BINDING; ANALOGS;

D O I：

10.1039/c3ob40377g

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

4H-1,4-oxazines were designed as transthyretin (TTR) amyloid fibril inhibitors based on an analysis of the interactions between known small molecule inhibitors and TTR by molecular docking. A series of 2,4,6-triaryl-4H-1,4-oxazines was synthesized by the cyclization of N,N-bis(phenacyl)anilines with POCl3 in pyridine. Inhibition of TTR amyloid fibril was evaluated by a fibril formation assay. The results indicate that 4H-1,4-oxazines significantly inhibit T'TR amyloid fibril at a concentration of 7.2 mu M.

引用

页码：4546 / 4550

页数：5

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