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Synthesis, Biological Evaluation, and Molecular Docking Studies of Xanthone Sulfonamides as ACAT Inhibitors
Author(s) -
Li Xiang,
Zou Yan,
Zhao Qingjie,
Yang Yan,
Wu Maocheng,
Huang Ting,
Hu Honggang,
Wu Qiuye
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12419
Subject(s) - xanthone , sterol o acyltransferase , docking (animal) , chemistry , stereochemistry , biochemistry , cholesterol , lipoprotein , medicine , nursing
Three series of xanthone sulfonamides were synthesized, and their inhibitory activities against acyl‐ C o A : cholesterol acyltransferase ( ACAT ) were evaluated. Results showed that most of the title compounds exhibited strong inhibitory activity against ACAT , of which compounds 1c , 1e , 1f , 2d , 2e, and 3d were proved to be more active than the positive control S andoz 58‐035. Computational docking experiments indicated that the interaction between inhibitors and ACAT contained the H ‐bond interaction, the hydrophobic interaction, and the narrow hydrophobic cleft.
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