Berberine Analogues as a novel class of the low-density-lipoprotein receptor up-regulators: synthesis, structure− activity relationships, and cholesterol-lowering …

YH Li, P Yang, WJ Kong, YX Wang, CQ Hu…

Index: Li, Ying-Hong; Yang, Peng; Kong, Wei-Jia; Wang, Yan-Xiang; Hu, Chang-Qin; Zuo, Zeng-Yan; Wang, Yue-Ming; Gao, Hong; Gao, Li-Mei; Feng, Yan-Chun; Du, Na-Na; Liu, Ying; Song, Dan-Qing; Jiang, Jian-Dong Journal of Medicinal Chemistry, 2009 , vol. 52, # 2 p. 492 - 501

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Citation Number: 55

Abstract

Twenty-nine derivatives of berberine (1) or pseudoberberine (2) were designed, semisynthesized, and evaluated for their up-regulatory activity on the low-density-lipoprotein receptor (LDLR) expression. SAR analysis revealed that (i) the methylenedioxy group at the 2-and 3-position is an essential element to keep the activity,(ii) the 7-position quaternary ammonium and planar structure of the compound are activity-required, and (iii) addition of ...