42833-68-1Relevant academic research and scientific papers
Discovery of novel xanthone derivatives as xanthine oxidase inhibitors
Hu, Lina,Hu, Honggang,Wu, Weifeng,Chai, Xiaoyun,Luo, Jianfei,Wu, Qiuye
scheme or table, p. 4013 - 4015 (2011/08/02)
Xanthine oxidase is the key enzyme that catalyzes the oxidation of hypoxanthine to xanthine and then to uric acid. In this study, a series of xanthone derivatives were synthesized as effective and a new class of xanthine oxidase inhibitor. Compounds 8a, 8c, 8i, 8g and 8r showed good inhibition against xanthine oxidase. The presence of a cyano group at the para position of benzyl moiety turned out to be the preferred substitution pattern. Molecular modeling studies were performed to gain an insight into its binding mode with xanthine oxidase, and to provide the basis for further structure-guided design of new non-purine xanthine oxidase inhibitors associated with the xanthone framework.
First identification of xanthone sulfonamides as potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors
Hu, Honggang,Liao, Hongli,Zhang, Jun,Wu, Weifeng,Yan, Jufang,Yan, Yonghong,Zhao, Qingjie,Zou, Yan,Chai, Xiaoyun,Yu, Shichong,Wu, Qiuye
scheme or table, p. 3094 - 3097 (2010/07/18)
Inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT) would be useful anti-atherogenic agents, since an absence of ACAT affects the absorption and transformation of cholesterol, indirectly resulting in the reduction of cholesteryl ester accumulation in blood vessels. This report discloses xanthone sulfonamides as novel class small molecule inhibitors of ACAT. A series of xanthone sulfonamides were synthesized and evaluated to result in the identification of several potent ACAT inhibitors, among which 2n proved to be more potent than the positive control Sandoz58-35. Moreover, a molecular model for the binding between 2n and the active site of ACAT-2 was provided based computational docking results.
γ-Pyrone compounds. II: Synthesis and antiplatelet effects of tetraoxygenated xanthones
Lin,Liou,Ko,Teng
, p. 1109 - 1112 (2007/10/02)
Norathyriol and its analogues, 1,3,5,6-, 3,4,5,6-, 3,4,6,7- and 2,3,6,7- tetrahydroxyxanthone, were synthesized from benzophenone precursors by Friedel-Crafts acylation and subsequent base-catalyzed cyclization to eliminate methanol. Both 3,4,6,7- and 2,3,6,7-tetrahydroxyxanthone tetraacetate showed potent anti-platelet aggregation effects on arachidonic acid-induced platelet aggregation. 3,4,6,7-Tetrahydroxyxanthone tetraacetate and 1,3,5,6-tetrahydroxyxanthone showed potent and significant anti-platelet aggregation effects on collagen-induced platelet aggregation.
Studies in the Xanthone Series. Part 13. Structural and Synthetic Studies on Toxyloxanthone B
Cotterill, Phillip J.,Scheinmann, Feodor
, p. 2353 - 2357 (2007/10/02)
A re-consideration of the 1H n.m.r. data for toxyloxanthone B trimethyl ether and an unambiguous total synthesis both show that toxyloxanthone B has the 1,1-dimethylpyranoxanthone structure (1a) and not the 3,3-dimethylpyranoxanthone system (2) previously assigned.The synthesis is based on the preparation of 1,7-dihydroxy-3,5-dimethoxyxanthone (5) from cyclisation of a benzophenone precursor (3a) or (3b) and selective demethylations.A Claisen rearrangement of the 7-prop-2-ynyloxyxanthone (6) followed by cyclisation and methylation gives toxyloxanthone B trimethyl ether.
