Literature DB >> 12067561

CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships.

Dean A Wacker1, Joseph B Santella, Daniel S Gardner, Jeffrey G Varnes, Melissa Estrella, George V DeLucca, Soo S Ko, Keiichi Tanabe, Paul S Watson, Patricia K Welch, Maryanne Covington, Nicole C Stowell, Eric A Wadman, Paul Davies, Kimberly A Solomon, Robert C Newton, George L Trainor, Steven M Friedman, Carl P Decicco, John V Duncia.   

Abstract

CCR3 antagonist leads with IC(50) values in the microM range were converted into low nM binding compounds that displayed in vitro inhibition of human eosinophil chemotaxis induced by human eotaxin. In particular, 4-benzylpiperidin-1-yl-n-propylureas and erythro-3-(4-benzyl-2-(alpha-hydroxyalkyl)piperidin-1-yl)-n-propylureas (obtained via Beak reaction of N-BOC-4-benzylpiperidine) exhibited single digit nanomolar IC(50) values for CCR3.

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Year:  2002        PMID: 12067561     DOI: 10.1016/s0960-894x(02)00206-8

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


  3 in total

1.  The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

Authors:  Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal:  Br J Pharmacol       Date:  2013-12       Impact factor: 8.739

2.  Ligand-based molecular design of 4-benzylpiperidinealkylureas and amides as CCR3 antagonists.

Authors:  Vaibhav Jain; Ashish Pandey; Shikhar Gupta; C Gopi Mohan
Journal:  J Mol Model       Date:  2009-12-04       Impact factor: 1.810

3.  CCR9 Is a Key Regulator of Early Phases of Allergic Airway Inflammation.

Authors:  C López-Pacheco; G Soldevila; G Du Pont; R Hernández-Pando; E A García-Zepeda
Journal:  Mediators Inflamm       Date:  2016-10-04       Impact factor: 4.711

  3 in total

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