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Literature DB >> 15357970

Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors.

Rune Ringom¹, Eva Axen, Jonas Uppenberg, Thomas Lundbäck, Lena Rondahl, Tjeerd Barf.

Abstract

The synthesis and biological evaluation of novel human A-FABP inhibitors based on the 6-(trifluoromethyl)pyrimidine-4(1H)-one scaffold is described. Two series of compounds, bearing either an amino or carbon substituent in the 2-position of the pyrimidine ring were investigated. Modification of substituents and chain length optimization led to novel compounds with low micromolar activity and good selectivity for human A-FABP.

Entities: Chemical Gene Species

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Year: 2004 PMID： 15357970 DOI： 10.1016/j.bmcl.2004.06.058

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

14 in total

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3. Interaction Analysis of FABP4 Inhibitors by X-ray Crystallography and Fragment Molecular Orbital Analysis.

Authors: Uno Tagami; Kazutoshi Takahashi; Shunsuke Igarashi; Chieko Ejima; Tomomi Yoshida; Sen Takeshita; Wataru Miyanaga; Masayuki Sugiki; Munetaka Tokumasu; Toshihiro Hatanaka; Tatsuki Kashiwagi; Kohki Ishikawa; Hiroshi Miyano; Toshimi Mizukoshi
Journal: ACS Med Chem Lett Date: 2016-02-16 Impact factor: 4.345

4. Calcium-dependent release of adipocyte fatty acid binding protein from human adipocytes.

Authors: I Schlottmann; M Ehrhart-Bornstein; M Wabitsch; S R Bornstein; V Lamounier-Zepter
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5. Benzbromarone, an old uricosuric drug, inhibits human fatty acid binding protein 4 in vitro and lowers the blood glucose level in db/db mice.

Authors: Hai-yan Cai; Ting Wang; Jian-chun Zhao; Peng Sun; Gui-rui Yan; Hai-peng Ding; Ying-xia Li; He-yao Wang; Wei-liang Zhu; Kai-xian Chen
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6. Small-molecule inhibitors of FABP4/5 ameliorate dyslipidemia but not insulin resistance in mice with diet-induced obesity.

Authors: Hong Lan; Cliff C Cheng; Timothy J Kowalski; Ling Pang; Lixin Shan; Cheng-Chi Chuang; James Jackson; Alberto Rojas-Triana; Loretta Bober; Li Liu; Johannes Voigt; Peter Orth; Xianshu Yang; Gerald W Shipps; Joseph A Hedrick
Journal: J Lipid Res Date: 2011-02-04 Impact factor: 5.922

Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors.

1. BMS309403 directly suppresses cardiac contractile function.

2. Structural analysis of ibuprofen binding to human adipocyte fatty-acid binding protein (FABP4).

3. Interaction Analysis of FABP4 Inhibitors by X-ray Crystallography and Fragment Molecular Orbital Analysis.

4. Calcium-dependent release of adipocyte fatty acid binding protein from human adipocytes.

5. Benzbromarone, an old uricosuric drug, inhibits human fatty acid binding protein 4 in vitro and lowers the blood glucose level in db/db mice.

6. Small-molecule inhibitors of FABP4/5 ameliorate dyslipidemia but not insulin resistance in mice with diet-induced obesity.

7. Expression, purification, crystallization and structure of human adipocyte lipid-binding protein (aP2).

Review 8. Fatty acid-binding proteins: role in metabolic diseases and potential as drug targets.

Review 9. Adipocyte/macrophage fatty acid binding proteins in metabolic syndrome.

10. Lipid chaperones and metabolic inflammation.