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Molecules 2013, 18(2), 1933-1948; doi:10.3390/molecules18021933

Design, Synthesis and Hepatoprotective Activity of Analogs of the Natural Product Goodyeroside A

1
State Key Laboratory of Bioactive Substance and Function of Natural Medicines & Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China
2
Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China
*
Author to whom correspondence should be addressed.
Received: 21 December 2012 / Revised: 29 January 2013 / Accepted: 30 January 2013 / Published: 1 February 2013
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Goodyeroside A, a natural product isolated from the Goodyera species, possesses significant hepatoprotective activity and has a novel skeleton not previously observed in other synthetic drugs used for the treatment of hepatitis. Herein, we report a highly stereoselective synthesis of goodyeroside A and related analogs with varying substituents at the α position of the carbonyl group to explore the structure-activity relationships of goodyeroside A. The absolute configuration of analog 5d was confirmed by single crystal X-ray analysis. The results from in vitro and in vivo studies indicate that 5a, the fully acetylated compound of goodyeroside A, is worthy of further investigation as a lead to identify novel hepatoprotective agents.
Keywords: goodyeroside A; structure-activity relationships; stereoselective; single crystal X-ray goodyeroside A; structure-activity relationships; stereoselective; single crystal X-ray
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Zhang, F.; Han, B.; Li, P.; Lin, Z.; Yin, D.; Li, Y.; Zhong, J.; Huang, H. Design, Synthesis and Hepatoprotective Activity of Analogs of the Natural Product Goodyeroside A. Molecules 2013, 18, 1933-1948.

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