Structural development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved aqueous solubility. Issue 4 (15th February 2018)

• Record Type: Journal Article
• Authors: Nomura, Sayaka; Endo-Umeda, Kaori; Fujii, Shinya; Makishima, Makoto; Hashimoto, Yuichi; Ishikawa, Minoru
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 4(2018)
• Page Start: 796
• Page End: 801
• Publication Date: 2018-02-15
• Subjects: Liver X receptor -- LXR -- Selective agonist; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.12.024
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.