학술논문

Design, Synthesis and Hepatoprotective Activity of Analogs of the Natural Product Goodyeroside A
Document Type
article
Source
Molecules, Vol 18, Iss 2, Pp 1933-1948 (2013)
Subject
goodyeroside A
structure-activity relationships
stereoselective
single crystal X-ray
Organic chemistry
QD241-441
Language
English
ISSN
1420-3049
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.