Structural development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved aqueous solubility

Sayaka Nomura, Kaori Endo-Umeda, Shinya Fujii, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

LXRβ-selective agonists are promising candidates to improve atherosclerosis without increasing plasma or hepatic TG levels. We have reported a series of tetrachlorophthalimide analogs as an LXRβ-selective agonist. However, they exhibited poor aqueous solubility probably due to its high hydrophobicity and highly rigid and plane structure. In this report, we present further structural development of tetrachloro(styrylphenyl)phthalimides as the LXRβ-selective agonists with improved aqueous solubility.

Original languageEnglish
Pages (from-to)796-801
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume28
Issue number4
DOIs
Publication statusPublished - 2018 Feb 15
Externally publishedYes

Keywords

  • LXR
  • Liver X receptor
  • Selective agonist

ASJC Scopus subject areas

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

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