Literature DB >> 23116889

Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H₁ antagonists. Part II: optimising in vivo clearance.

Mark Furber1, Lilian Alcaraz, Christopher Luckhurst, Ash Bahl, Haydn Beaton, Keith Bowers, John Collington, Rebecca Denton, David Donald, Elizabeth Kinchin, Cathy MacDonald, Aaron Rigby, Rob Riley, Matt Soars, Brian Springthorpe, Peter Webborn.   

Abstract

The second part of this communication focuses on the resolution of issues surrounding the series of hydroxyamide phenoxypiperidine CCR3/H(1) dual antagonists described in Part I. This involved further structural exploration directed at reducing metabolism and leading to the identification of compound 60 with a greatly improved in vivo pharmacokinetic profile.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23116889     DOI: 10.1016/j.bmcl.2012.09.112

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


  1 in total

1.  Isoquinolone-4-Carboxylic Acids by Ammonia-Ugi-4CR and Copper-Catalyzed Domino Reaction.

Authors:  Qian Wang; Kumchok C Mgimpatsang; Xin Li; Alexander Dömling
Journal:  J Org Chem       Date:  2021-06-29       Impact factor: 4.354

  1 in total

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