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Issue 27, 2013
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Synthesis of 4H-1,4-oxazines as transthyretin amyloid fibril inhibitors

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Abstract

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 TTR amyloid fibril at a concentration of 7.2 μM.

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

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Publication details

The article was received on 21 Feb 2013, accepted on 15 May 2013 and first published on 15 May 2013


Article type: Paper
DOI: 10.1039/C3OB40377G
Citation: Org. Biomol. Chem., 2013,11, 4546-4550
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    Synthesis of 4H-1,4-oxazines as transthyretin amyloid fibril inhibitors

    W. Li, X. Duan, H. Yan and H. Xin, Org. Biomol. Chem., 2013, 11, 4546
    DOI: 10.1039/C3OB40377G

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