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Structural development of tetrachlorophthalimides as liver X receptor ß (LXRß)-selective agonists with improved aqueous solubility.
Nomura, Sayaka; Endo-Umeda, Kaori; Fujii, Shinya; Makishima, Makoto; Hashimoto, Yuichi; Ishikawa, Minoru.
Affiliation
  • Nomura S; Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
  • Endo-Umeda K; Nihon University School of Medicine, 30-1 Oyaguchi-kamicho, Itabashi-ku, Tokyo 173-8610, Japan.
  • Fujii S; Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
  • Makishima M; Nihon University School of Medicine, 30-1 Oyaguchi-kamicho, Itabashi-ku, Tokyo 173-8610, Japan.
  • Hashimoto Y; Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
  • Ishikawa M; Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan. Electronic address: m-ishikawa@iam.u-tokyo.ac.jp.
Bioorg Med Chem Lett ; 28(4): 796-801, 2018 02 15.
Article in En | MEDLINE | ID: mdl-29398545
ABSTRACT
LXRß-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 LXRß-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 LXRß-selective agonists with improved aqueous solubility.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Phthalimides / Water / Liver X Receptors Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2018 Type: Article Affiliation country: Japan
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Phthalimides / Water / Liver X Receptors Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2018 Type: Article Affiliation country: Japan