Literature DB >> 17553678

Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists.

Yukiyoshi Yamazaki1, Kazutoyo Abe, Tsutomu Toma, Masahiro Nishikawa, Hidefumi Ozawa, Ayumu Okuda, Takaaki Araki, Soichi Oda, Keisuke Inoue, Kimiyuki Shibuya, Bart Staels, Jean-Charles Fruchart.   

Abstract

A combination of benzoxazole, phenoxyalkyl side chain, and phenoxybutyric acids was identified as a highly potent and selective human peroxisome proliferator-activated receptor alpha (PPARalpha) agonist. The synthesis, structure-activity relationship (SAR) studies, and in vivo activities of the representative compounds are described.

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Year:  2007        PMID： 17553678     DOI： 10.1016/j.bmcl.2007.05.066

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


  24 in total

1.  Transcriptome Analysis of K-877 (a Novel Selective PPARα Modulator (SPPARMα))-Regulated Genes in Primary Human Hepatocytes and the Mouse Liver.

Authors:  Sana Raza-Iqbal; Toshiya Tanaka; Motonobu Anai; Takeshi Inagaki; Yoshihiro Matsumura; Kaori Ikeda; Akashi Taguchi; Frank J Gonzalez; Juro Sakai; Tatsuhiko Kodama
Journal:  J Atheroscler Thromb       Date:  2015-06-04       Impact factor: 4.928

2.  Systems Approach to Discovery of Therapeutic Targets for Vein Graft Disease: PPARα Pivotally Regulates Metabolism, Activation, and Heterogeneity of Macrophages and Lesion Development.

Authors:  Julius L Decano; Sasha A Singh; Cauê Gasparotto Bueno; Lang Ho Lee; Arda Halu; Sarvesh Chelvanambi; Joan T Matamalas; Hengmin Zhang; Andrew K Mlynarchik; Jiao Qiao; Amitabh Sharma; Shin Mukai; Jianguo Wang; Daniel G Anderson; C Keith Ozaki; Peter Libby; Elena Aikawa; Masanori Aikawa
Journal:  Circulation       Date:  2021-04-06       Impact factor: 39.918

3.  A Novel Selective PPARα Modulator (SPPARMα), K-877 (Pemafibrate), Attenuates Postprandial Hypertriglyceridemia in Mice.

Authors:  Masami Sairyo; Takuya Kobayashi; Daisaku Masuda; Koutaro Kanno; Yinghong Zhu; Takeshi Okada; Masahiro Koseki; Tohru Ohama; Makoto Nishida; Yasushi Sakata; Shizuya Yamashita
Journal:  J Atheroscler Thromb       Date:  2017-08-05       Impact factor: 4.928

Review 4.  Alzheimer's Disease, a Lipid Story: Involvement of Peroxisome Proliferator-Activated Receptor α.

Authors:  Francisco Sáez-Orellana; Jean-Noël Octave; Nathalie Pierrot
Journal:  Cells       Date:  2020-05-14       Impact factor: 6.600

Review 5.  The Opportunities and Challenges of Peroxisome Proliferator-Activated Receptors Ligands in Clinical Drug Discovery and Development.

Authors:  Fan Hong; Pengfei Xu; Yonggong Zhai
Journal:  Int J Mol Sci       Date:  2018-07-27       Impact factor: 5.923

6.  Pemafibrate Protects against Fatty Acid-Induced Nephropathy by Maintaining Renal Fatty Acid Metabolism.

Authors:  Daiki Aomura; Makoto Harada; Yosuke Yamada; Takero Nakajima; Koji Hashimoto; Naoki Tanaka; Yuji Kamijo
Journal:  Metabolites       Date:  2021-06-09

Review 7.  Selective peroxisome proliferator-activated receptor α modulators (SPPARMα): the next generation of peroxisome proliferator-activated receptor α-agonists.

Authors:  Jean-Charles Fruchart
Journal:  Cardiovasc Diabetol       Date:  2013-05-31       Impact factor: 9.951

Review 8.  Pemafibrate (K-877), a novel selective peroxisome proliferator-activated receptor alpha modulator for management of atherogenic dyslipidaemia.

Authors:  Jean-Charles Fruchart
Journal:  Cardiovasc Diabetol       Date:  2017-10-04       Impact factor: 9.951

Review 9.  Selective Peroxisome Proliferator-Activated Receptor Alpha Modulators (SPPARMα): New Opportunities to Reduce Residual Cardiovascular Risk in Chronic Kidney Disease?

Authors:  Jean-Charles Fruchart; Michel P Hermans; Jamila Fruchart-Najib
Journal:  Curr Atheroscler Rep       Date:  2020-07-15       Impact factor: 5.113

10.  The Peroxisome Proliferator-Activated Receptor α (PPARα) Agonist Pemafibrate Protects against Diet-Induced Obesity in Mice.

Authors:  Masaya Araki; Yoshimi Nakagawa; Asayo Oishi; Song-Iee Han; Yunong Wang; Kae Kumagai; Hiroshi Ohno; Yuhei Mizunoe; Hitoshi Iwasaki; Motohiro Sekiya; Takashi Matsuzaka; Hitoshi Shimano
Journal:  Int J Mol Sci       Date:  2018-07-23       Impact factor: 5.923
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