Literature DB >> 22094028

Lead optimisation of pyrazoles as novel FPR1 antagonists.

Andrew D Morley1, Sarah King, Bryan Roberts, Sarah Lever, Barry Teobald, Adrian Fisher, Tony Cook, Beth Parker, Mark Wenlock, Caroline Phillips, Ken Grime.   

Abstract

Optimisation of a series of pyrazole inhibitors of the human FPR1 receptor has been achieved. The use of an in vitro media loss assay was utilised to identify sub-series with more robust DMPK profiles. These were subsequently improved to generate analogues with attractive overall profiles.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 22094028     DOI： 10.1016/j.bmcl.2011.10.090

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


  6 in total

1.  Selective agonists and antagonists of formylpeptide receptors: duplex flow cytometry and mixture-based positional scanning libraries.

Authors:  Clemencia Pinilla; Bruce S Edwards; Jon R Appel; Tina Yates-Gibbins; Marc A Giulianotti; Jose L Medina-Franco; Susan M Young; Radleigh G Santos; Larry A Sklar; Richard A Houghten
Journal:  Mol Pharmacol       Date:  2013-06-20       Impact factor: 4.436

2.  Antagonism of human formyl peptide receptor 1 (FPR1) by chromones and related isoflavones.

Authors:  Igor A Schepetkin; Liliya N Kirpotina; Andrei I Khlebnikov; Ni Cheng; Richard D Ye; Mark T Quinn
Journal:  Biochem Pharmacol       Date:  2014-10-17       Impact factor: 5.858

Review 3.  Development of small molecule non-peptide formyl peptide receptor (FPR) ligands and molecular modeling of their recognition.

Authors:  I A Schepetkin; A I Khlebnikov; M P Giovannoni; L N Kirpotina; A Cilibrizzi; M T Quinn
Journal:  Curr Med Chem       Date:  2014       Impact factor: 4.530

4.  Novel 3-(1H-indol-3-yl)-2-[3-(4-methoxyphenyl)ureido]propanamides as selective agonists of human formyl-peptide receptor 2.

Authors:  Enza Lacivita; Igor A Schepetkin; Madia L Stama; Liliya N Kirpotina; Nicola A Colabufo; Roberto Perrone; Andrei I Khlebnikov; Mark T Quinn; Marcello Leopoldo
Journal:  Bioorg Med Chem       Date:  2014-12-13       Impact factor: 3.641

5.  Aurantiamide-related dipeptide derivatives are formyl peptide receptor 1 antagonists.

Authors:  Margherita Mastromarino; Liliya N Kirpotina; Igor A Schepetkin; Mark T Quinn; Enza Lacivita; Marcello Leopoldo
Journal:  Medchemcomm       Date:  2019-10-07       Impact factor: 3.597

6.  Application of small molecule FPR1 antagonists in the treatment of cancers.

Authors:  Djevdet S Ahmet; Haneen A Basheer; Anwar Salem; Di Lu; Amin Aghamohammadi; Patrick Weyerhäuser; Andrea Bordiga; Juman Almeniawi; Sabah Rashid; Patricia A Cooper; Steven D Shnyder; Victoria Vinader; Kamyar Afarinkia
Journal:  Sci Rep       Date:  2020-10-14       Impact factor: 4.379
  6 in total

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