Literature DB >> 20207151

Novel acyl coenzyme A (CoA): diacylglycerol acyltransferase-1 inhibitors: synthesis and biological activities of diacylethylenediamine derivatives.

Yoshihisa Nakada1, Thomas D Aicher, Yvan Le Huerou, Timothy Turner, Scott A Pratt, Stephen S Gonzales, Steve A Boyd, Hiroshi Miki, Toshihiro Yamamoto, Hiroshi Yamaguchi, Koki Kato, Shuji Kitamura.   

Abstract

A series of diacylethylenediamine derivatives were synthesized and evaluated for their inhibitory activity against DGAT-1 and pharmacokinetic profile to discover new small molecule DGAT-1 inhibitors. Among the compounds, N-[2-({[1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]carbonyl}amino)ethyl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide 3x showed potent inhibitory activity and excellent PK profile. Oral administration of 3x to mice with dietary-induced obesity resulted in reduced body weight gain and white adipose tissue weight. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20207151     DOI： 10.1016/j.bmc.2010.01.067

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


  5 in total

Review 1.  Mammalian triacylglycerol metabolism: synthesis, lipolysis, and signaling.

Authors:  Rosalind A Coleman; Douglas G Mashek
Journal:  Chem Rev       Date:  2011-06-01       Impact factor: 60.622

Review 2.  Chemical modulation of glycerolipid signaling and metabolic pathways.

Authors:  Sarah A Scott; Thomas P Mathews; Pavlina T Ivanova; Craig W Lindsley; H Alex Brown
Journal:  Biochim Biophys Acta       Date:  2014-01-15

3.  DGAT1 mutation is linked to a congenital diarrheal disorder.

Authors:  Joel T Haas; Harland S Winter; Elaine Lim; Andrew Kirby; Brendan Blumenstiel; Matthew DeFelice; Stacey Gabriel; Chaim Jalas; David Branski; Carrie A Grueter; Mauro S Toporovski; Tobias C Walther; Mark J Daly; Robert V Farese
Journal:  J Clin Invest       Date:  2012-11-01       Impact factor: 14.808

4.  Investigation of an 18F-labelled Imidazopyridotriazine for Molecular Imaging of Cyclic Nucleotide Phosphodiesterase 2A.

Authors:  Susann Schröder; Barbara Wenzel; Winnie Deuther-Conrad; Rodrigo Teodoro; Mathias Kranz; Matthias Scheunemann; Ute Egerland; Norbert Höfgen; Detlef Briel; Jörg Steinbach; Peter Brust
Journal:  Molecules       Date:  2018-03-02       Impact factor: 4.411

5.  Synthesis and antifungal activity of N-(substituted pyridinyl)-1-methyl(phenyl)-3-(trifluoromethyl)-1H-pyrazole-4-carboxamide derivatives.

Authors:  Zhibing Wu; Deyu Hu; Jiqing Kuang; Hua Cai; Shixi Wu; Wei Xue
Journal:  Molecules       Date:  2012-11-30       Impact factor: 4.411
  5 in total

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