文献类型：期刊文献

英文题名：Synthesis, modification, and evaluation of (R)-de-O-methyllasiodiplodin and analogs as nonsteroidal antagonists of mineralocorticoid receptor

作者：Jiang, Cheng-Shi[1];Zhou, Rong[2];Gong, Jing-Xu[1];Chen, Li-Li[1];Kurtan, Tibor[3];Shen, Xu[1,2];Guo, Yue-Wei[1]

机构：[1]Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;[2]E China Univ Sci & Technol, Shanghai 200237, Peoples R China;[3]Univ Debrecen, Dept Organ Chem, H-4010 Debrecen, Hungary

年份：2011

卷号：21

期号：4

起止页码：1171

外文期刊名：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000286972400018)】；

基金：This research work was financially supported by National S & T Major Project (Nos. 2009ZX09301-001, 2009ZX09103-060), National Marine 863 Programme for Druggability Evaluation (2011-2013), Natural Science Foundation of China (Nos. 30730108, 40976048, 81072572), STCSM Project (09ZR1438000, 10540702900), CAS Key Project (SIMM0907KF-09), and partially funded by grant from CAS (KSCX2-YW-R-18).

语种：英文

外文关键词：Macrolide; (R)-De-O-methyllasiodiplodin; Mineralocorticoid receptor; Antagonist; Ring-closing-metathesis reaction

摘要：Macrolide (R)-de-O-methyllasiodiplodin (1), discovered to be a potent nonsteroidal antagonist of the mineralocorticoid receptor (MR), was synthesized via an efficient method and evaluated for MR antagonistic activity together with its analogs. Among all the tested compounds, compounds 18a, 18b and 18c, exhibited more potent antagonistic activity against MR with IC50 values ranging from 0.58 to 1.11 mu M. Generally, it was obviously demonstrated that acetylation at phenolic hydroxyl groups and the ring size in analogs of 1 were very important for MR antagonist activity. (c) 2010 Elsevier Ltd. All rights reserved.