title: Synthesis of 4H-1,4-oxazines as transthyretin amyloid fibril inhibitors.
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.
authors.affiliation: College of Life Science and Bio-engineering, Beijing University of Technology, Pingleyuan Street No. 100, Chaoyang District, Beijing 100124, PR China.
authors.forename: Weipeng
authors.initials: W
authors.lastname: Li
authors.forename: Xiaowei
authors.initials: X
authors.lastname: Duan
authors.forename: Hong
authors.initials: H
authors.lastname: Yan
authors.forename: Hongxing
authors.initials: H
authors.lastname: Xin
mesh_terms: D000682:Amyloid / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D006801:Humans; D062105:Molecular Docking Simulation; D010078:Oxazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011228:Prealbumin / Q000737:chemistry / Q000378:metabolism*
chemical_list: D000682:Amyloid; D010078:Oxazines; D011228:Prealbumin