Literature DB >> 20801037

Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.

Mark R Herbert1, Dana L Siegel, Lena Staszewski, Charmagne Cayanan, Urmi Banerjee, Sangeeta Dhamija, Jennifer Anderson, Amy Fan, Li Wang, Peter Rix, Andrew K Shiau, Tadimeti S Rao, Stewart A Noble, Richard A Heyman, Eric Bischoff, Mausumee Guha, Ayman Kabakibi, Anthony B Pinkerton.   

Abstract

Optimization of a screening hit from uHTS led to the discovery of TGR5 agonist 32, which was shown to have activity in a rodent model for diabetes.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20801037     DOI： 10.1016/j.bmcl.2010.08.014

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


  14 in total

Review 1.  The bile acid TGR5 membrane receptor: from basic research to clinical application.

Authors:  Henri Duboc; Yvette Taché; Alan F Hofmann
Journal:  Dig Liver Dis       Date:  2014-01-09       Impact factor: 4.088

2.  Probing the Binding Site of Bile Acids in TGR5.

Authors:  Antonio Macchiarulo; Antimo Gioiello; Charles Thomas; Thijs W H Pols; Roberto Nuti; Cristina Ferrari; Nicola Giacchè; Francesca De Franco; Mark Pruzanski; Johan Auwerx; Kristina Schoonjans; Roberto Pellicciari
Journal:  ACS Med Chem Lett       Date:  2013-10-15       Impact factor: 4.345

3.  Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.

Authors:  David W Piotrowski; Kentaro Futatsugi; Joseph S Warmus; Suvi T M Orr; Kevin D Freeman-Cook; Allyn T Londregan; Liuqing Wei; Sandra M Jennings; Michael Herr; Steven B Coffey; Wenhua Jiao; Gregory Storer; David Hepworth; Jian Wang; Sophie Y Lavergne; Janice E Chin; John R Hadcock; Martin B Brenner; Angela C Wolford; Ann M Janssen; Nicole S Roush; Joanne Buxton; Terri Hinchey; Amit S Kalgutkar; Raman Sharma; Declan A Flynn
Journal:  ACS Med Chem Lett       Date:  2012-11-09       Impact factor: 4.345

4.  Discovery of Orally Efficacious Tetrahydrobenzimidazoles as TGR5 Agonists for Type 2 Diabetes.

Authors:  Xuqing Zhang; Mark Wall; Zhihua Sui; Jack Kauffman; Cuifen Hou; Cailin Chen; Fuyong Du; Thomas Kirchner; Yin Liang; Dana L Johnson; William V Murray; Keith Demarest
Journal:  ACS Med Chem Lett       Date:  2017-04-21       Impact factor: 4.345

5.  TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading.

Authors:  Thijs W H Pols; Mitsunori Nomura; Taoufiq Harach; Giuseppe Lo Sasso; Maaike H Oosterveer; Charles Thomas; Giovanni Rizzo; Antimo Gioiello; Luciano Adorini; Roberto Pellicciari; Johan Auwerx; Kristina Schoonjans
Journal:  Cell Metab       Date:  2011-12-07       Impact factor: 27.287

Review 6.  Bile acid receptors as targets for the treatment of dyslipidemia and cardiovascular disease.

Authors:  Geoffrey Porez; Janne Prawitt; Barbara Gross; Bart Staels
Journal:  J Lipid Res       Date:  2012-05-01       Impact factor: 5.922

Review 7.  Pleiotropic functions of the organic solute transporter Ostα-Ostβ.

Authors:  Nazzareno Ballatori
Journal:  Dig Dis       Date:  2011-06-17       Impact factor: 2.404

Review 8.  The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation.

Authors:  Thijs W H Pols; Lilia G Noriega; Mitsunori Nomura; Johan Auwerx; Kristina Schoonjans
Journal:  J Hepatol       Date:  2010-12-09       Impact factor: 25.083

Review 9.  Pharmacological approaches to restore mitochondrial function.

Authors:  Pénélope A Andreux; Riekelt H Houtkooper; Johan Auwerx
Journal:  Nat Rev Drug Discov       Date:  2013-05-13       Impact factor: 84.694

10.  Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist.

Authors:  Sameer Agarwal; Amit Patil; Umesh Aware; Prashant Deshmukh; Brijesh Darji; Santosh Sasane; Kalapatapu V V M Sairam; Priyanka Priyadarsiny; Poonam Giri; Harilal Patel; Suresh Giri; Mukul Jain; Ranjit C Desai
Journal:  ACS Med Chem Lett       Date:  2015-11-20       Impact factor: 4.345
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