Literature DB >> 19539483

Separation of alpha-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXRalpha-selective antagonists.

Kazunori Motoshima1, Tomomi Noguchi-Yachide, Kazuyuki Sugita, Yuichi Hashimoto, Minoru Ishikawa.   

Abstract

Liver X receptor (LXR) alpha/beta dual agonists are candidate medicaments for the treatment of metabolic syndrome, because their biological actions include increasing cholesterol efflux mediated by LXRbeta. However, their clinical application is currently limited by their enhancing effect on triglyceride (TG) synthesis mediated by LXRalpha. Combination of an LXRalpha-selective antagonist with an LXRalpha/beta dual agonist may overcome this disadvantage. In the present work, structural development studies of phenethylphenyl phthalimide 9, which possesses LXRalpha/beta dual-antagonistic activity and alpha-glucosidase-inhibitory activity, led to the LXRalpha-selective antagonist 23f. Specific alpha-glucosidase inhibitors were also obtained.

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Year:  2009        PMID： 19539483     DOI： 10.1016/j.bmc.2009.05.066

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  11 in total

1.  Design, synthesis, and biological evaluation of resveratrol analogues as aromatase and quinone reductase 2 inhibitors for chemoprevention of cancer.

Authors:  Bin Sun; Juma Hoshino; Katie Jermihov; Laura Marler; John M Pezzuto; Andrew D Mesecar; Mark Cushman
Journal:  Bioorg Med Chem       Date:  2010-05-24       Impact factor: 3.641

2.  Borylated 2,3,4,5-Tetrachlorophthalimide and Their 2,3,4,5-Tetrachlorobenzamide Analogues: Synthesis, Their Glycosidase Inhibition and Anticancer Properties in View to Boron Neutron Capture Therapy.

Authors:  David M Campkin; Yuna Shimadate; Barbara Bartholomew; Paul V Bernhardt; Robert J Nash; Jennette A Sakoff; Atsushi Kato; Michela I Simone
Journal:  Molecules       Date:  2022-05-26       Impact factor: 4.927

3.  Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.

Authors:  Sayaka Nomura; Kaori Endo-Umeda; Atsushi Aoyama; Makoto Makishima; Yuichi Hashimoto; Minoru Ishikawa
Journal:  ACS Med Chem Lett       Date:  2015-07-13       Impact factor: 4.345

4.  Promiscuous activity of the LXR antagonist GSK2033 in a mouse model of fatty liver disease.

Authors:  Kristine Griffett; Thomas P Burris
Journal:  Biochem Biophys Res Commun       Date:  2016-09-25       Impact factor: 3.575

Review 5.  Role of liver X receptors in cholesterol efflux and inflammatory signaling (review).

Authors:  Rongtao Zhu; Zhibing Ou; Xiongzhong Ruan; Jianping Gong
Journal:  Mol Med Rep       Date:  2012-01-17       Impact factor: 2.952

6.  2-{[(E)-2-Hy-droxy-benzyl-idene]amino}-1H-isoindole-1,3(2H)-dione.

Authors:  H C Devarajegowda; H D Revanasiddappa; L Shiva Kumar; V Sumangala; V D Jagadeesh Prasad
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-10-02

Review 7.  Expression and clinical significance of LXRα and SREBP-1c in placentas of preeclampsia.

Authors:  Li Jianhua; Miao Xueqin; Hu Jifen
Journal:  Open Med (Wars)       Date:  2016-08-13

8.  Efficient Lead Finding, Activity Enhancement and Preliminary Selectivity Control of Nuclear Receptor Ligands Bearing a Phenanthridinone Skeleton.

Authors:  Yuko Nishiyama; Shinya Fujii; Makoto Makishima; Yuichi Hashimoto; Minoru Ishikawa
Journal:  Int J Mol Sci       Date:  2018-07-18       Impact factor: 5.923

9.  Liver LXRα expression is crucial for whole body cholesterol homeostasis and reverse cholesterol transport in mice.

Authors:  Yuan Zhang; Sarah R Breevoort; Jerry Angdisen; Mingui Fu; Daniel R Schmidt; Sam R Holmstrom; Steven A Kliewer; David J Mangelsdorf; Ira G Schulman
Journal:  J Clin Invest       Date:  2012-04-09       Impact factor: 14.808

10.  Diaryl azo derivatives as anti-diabetic and antimicrobial agents: synthesis, in vitro, kinetic and docking studies.

Authors:  Tehreem Tahir; Mirza Imran Shahzad; Rukhsana Tabassum; Muhammad Rafiq; Muhammad Ashfaq; Mubashir Hassan; Katarzyna Kotwica-Mojzych; Mariusz Mojzych
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051
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