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

✍ Scribed by Cheng-Shi Jiang; Rong Zhou; Jing-Xu Gong; Li-Li Chen; Tibor Kurtán; Xu Shen; Yue-Wei Guo

• Book ID: 104005271
• Publisher: Elsevier Science
• Year: 2011
• Tongue: English
• Weight: 385 KB
• Volume: 21
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.12.101

✦ Synopsis

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 IC 50 values ranging from 0.58 to 1.11 lM. 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.