37884-02-9Relevant articles and documents
Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis
Kitakami, Ryota,Inui, Kishin,Nakagawa, Yusuke,Sawai, Yurika,Katayama, Wakana,Yokoyama, Takeshi,Okada, Takuya,Kanamitsu, Kayoko,Nakagawa, Shinsaku,Toyooka, Naoki,Mizuguchi, Mineyuki
, (2021/07/06)
Transthyretin is a tetrameric protein which functions as a transporter of thyroxine and retinol-binding protein. Misfolding and amyloid aggregation of transthyretin are known to cause wild-type and hereditary transthyretin amyloidosis. Stabilization of the transthyretin tetramer by low molecular weight compounds is an efficacious strategy to inhibit the aggregation pathway in the amyloidosis. Here, we investigated the inhibitory activities of anthraquinone and xanthone derivatives against amyloid aggregation, and found that xanthone-2-carboxylic acid with one chlorine or methyl group has strong inhibitory activity comparable with that of diflunisal, which is one of the best known stabilizers of transthyretin. X-ray crystallographic structures of transthyretin in complex with the compounds revealed that the introduction of chlorine, which is buried in a hydrophobic region, is important for the strong inhibitory effect of the stabilizer against amyloidogenesis. An in vitro absorption, distribution, metabolism and elimination (ADME) study and in vivo pharmacokinetic study demonstrated that the compounds have drug-like features, suggesting that they have potential as therapeutic agents to stabilize transthyretin.
XANTHONE DERIVATIVES, UV PROTECTIVE COMPOSITION CONCENTRATE, METHOD OF PREPARATION OF UV PROTECTIVE COMPOSITION CONCENTRATE, USE OF UV PROTECTIVE COMPOSITION CONCENTRATE AND COSMETIC UV PROTECTIVE PRODUCT
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Page/Page column 5, (2021/10/30)
The first object of the invention is a xanthone derivative described by formula (I) where R1 is a substituent selected from the group comprising: hydrogen or alkoxy group; R2 is a substituent selected from the group comprising methyl
Anticonvulsant evaluation of aminoalkanol derivatives of 2- and 4-methylxanthone
Szkaradek, Natalia,Gunia, Agnieszka,Waszkielewicz, Anna M.,Antkiewicz-Michaluk, Lucyna,Ceg?a, Marek,Szneler, Edward,Marona, Henryk
, p. 1190 - 1198 (2013/03/28)
A series of 17 new aminoalkanol derivatives of 6-methoxy- or 7-chloro-2-methylxanthone as well as 6-methoxy-4-methylxanthone was synthesized and evaluated for anticonvulsant activity. All compounds were verified in mice after intraperitoneal (ip) administ