Literature DB >> 20627722

Identification of a sulfonamide series of CCR2 antagonists.

Simon Peace1, Joanne Philp, Carl Brooks, Val Piercy, Kitty Moores, Chris Smethurst, Steve Watson, Simon Gaines, Mara Zippoli, Claudette Mookherjee, Robert Ife.   

Abstract

A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular moderation of lipophilicity and study of pK(a), yielded highly potent CCR2 antagonists exhibiting good pharmacokinetic properties and improved potency in the presence of human plasma. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20627722     DOI： 10.1016/j.bmcl.2010.04.142

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


  6 in total

1.  Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

Authors:  Chu-Biao Xue; Anlai Wang; Qi Han; Yingxin Zhang; Ganfeng Cao; Hao Feng; Taisheng Huang; Changsheng Zheng; Michael Xia; Ke Zhang; Lingquan Kong; Joseph Glenn; Rajan Anand; David Meloni; D J Robinson; Lixin Shao; Lou Storace; Mei Li; Robert O Hughes; Rajesh Devraj; Philip A Morton; D Joseph Rogier; Maryanne Covington; Peggy Scherle; Sharon Diamond; Tom Emm; Swamy Yeleswaram; Nancy Contel; Kris Vaddi; Robert Newton; Greg Hollis; Brian Metcalf
Journal:  ACS Med Chem Lett       Date:  2011-10-05       Impact factor: 4.345

Review 2.  What Do Structures Tell Us About Chemokine Receptor Function and Antagonism?

Authors:  Irina Kufareva; Martin Gustavsson; Yi Zheng; Bryan S Stephens; Tracy M Handel
Journal:  Annu Rev Biophys       Date:  2017-05-22       Impact factor: 12.981

3.  Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.

Authors:  Chu-Biao Xue; Hao Feng; Ganfeng Cao; Taisheng Huang; Joseph Glenn; Rajan Anand; David Meloni; Ke Zhang; Lingquan Kong; Anlai Wang; Yingxin Zhang; Changsheng Zheng; Michael Xia; Lihua Chen; Hiroyuki Tanaka; Qi Han; D J Robinson; Dilip Modi; Lou Storace; Lixin Shao; Vaqar Sharief; Mei Li; Laurine G Galya; Maryanne Covington; Peggy Scherle; Sharon Diamond; Tom Emm; Swamy Yeleswaram; Nancy Contel; Kris Vaddi; Robert Newton; Greg Hollis; Steven Friedman; Brian Metcalf
Journal:  ACS Med Chem Lett       Date:  2011-03-31       Impact factor: 4.345

Review 4.  Structural Analysis of Chemokine Receptor-Ligand Interactions.

Authors:  Marta Arimont; Shan-Liang Sun; Rob Leurs; Martine Smit; Iwan J P de Esch; Chris de Graaf
Journal:  J Med Chem       Date:  2017-03-10       Impact factor: 7.446

5.  Design and Characterization of an Intracellular Covalent Ligand for CC Chemokine Receptor 2.

Authors:  Natalia V Ortiz Zacarías; Kirti K Chahal; Tereza Šimková; Cas van der Horst; Yi Zheng; Asuka Inoue; Emy Theunissen; Lloyd Mallee; Daan van der Es; Julien Louvel; Adriaan P IJzerman; Tracy M Handel; Irina Kufareva; Laura H Heitman
Journal:  J Med Chem       Date:  2021-02-18       Impact factor: 7.446

6.  Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2.

Authors:  Natalia V Ortiz Zacarías; Jacobus P D van Veldhoven; Laura Portner; Eric van Spronsen; Salviana Ullo; Margo Veenhuizen; Wijnand J C van der Velden; Annelien J M Zweemer; Roy M Kreekel; Kenny Oenema; Eelke B Lenselink; Laura H Heitman; Adriaan P IJzerman
Journal:  J Med Chem       Date:  2018-10-11       Impact factor: 7.446
  6 in total

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