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

Cheng Shi Jiang, Rong Zhou, Jing Xu Gong, Li Li Chen, Tibor Kurtán, Xu Shen, Yue Wei Guo

Research output: Contribution to journalArticle

27 Citations (Scopus)

Abstract

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 μM. 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.

Original languageEnglish
Pages (from-to)1171-1175
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number4
DOIs
Publication statusPublished - Feb 15 2011

Keywords

  • (R)-De-O-methyllasiodiplodin
  • Antagonist
  • Macrolide
  • Mineralocorticoid receptor
  • Ring-closing-metathesis reaction

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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