Literature DB >> 12031318

CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors.

R P Alexander1, G J Warrellow, M A W Eaton, E C Boyd, J C Head, J R Porter, J A Brown, J T Reuberson, B Hutchinson, P Turner, B Boyce, D Barnes, B Mason, A Cannell, R J Taylor, A Zomaya, A Millican, J Leonard, R Morphy, M Wales, M Perry, R A Allen, N Gozzard, B Hughes, G Higgs.   

Abstract

The discovery, synthesis and biological activity of a series of triarylethane phosphodiesterase 4 inhibitors is described. Structure-activity relationship studies are presented for CDP840 (29), a potent, chiral, selective inhibitor of PDE 4 (IC(50) 4nM). CDP840 is non-emetic in the ferret at 30mgkg(-1) (po), active in models of inflammation and reverses ozone-induced bronchial hyperreactivity in the guinea pig.

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Year:  2002        PMID: 12031318     DOI: 10.1016/s0960-894x(02)00202-0

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


  7 in total

1.  Assessing protein-ligand binding modes with computational tools: the case of PDE4B.

Authors:  Gülşah Çifci; Viktorya Aviyente; E Demet Akten; Gerald Monard
Journal:  J Comput Aided Mol Des       Date:  2017-05-22       Impact factor: 3.686

2.  Deletion of phosphodiesterase 4D in mice shortens alpha(2)-adrenoceptor-mediated anesthesia, a behavioral correlate of emesis.

Authors:  Annette Robichaud; Panagiota B Stamatiou; S-L Catherine Jin; Nicholas Lachance; Dwight MacDonald; France Laliberté; Susana Liu; Zheng Huang; Marco Conti; Chi-Chung Chan
Journal:  J Clin Invest       Date:  2002-10       Impact factor: 14.808

3.  Development and Analysis of a Pd(0)-Catalyzed Enantioselective 1,1-Diarylation of Acrylates Enabled by Chiral Anion Phase Transfer.

Authors:  Eiji Yamamoto; Margaret J Hilton; Manuel Orlandi; Vaneet Saini; F Dean Toste; Matthew S Sigman
Journal:  J Am Chem Soc       Date:  2016-11-30       Impact factor: 15.419

4.  Palladium-catalyzed asymmetric allylic 4-pyridinylation via electroreductive substitution reaction.

Authors:  Weijie Ding; Mengfan Li; Jinkun Fan; Xu Cheng
Journal:  Nat Commun       Date:  2022-09-26       Impact factor: 17.694

Review 5.  ABCD of the phosphodiesterase family: interaction and differential activity in COPD.

Authors:  David M G Halpin
Journal:  Int J Chron Obstruct Pulmon Dis       Date:  2008

6.  Nickel-Catalyzed Asymmetric Reductive Diarylation of Vinylarenes.

Authors:  David Anthony; Qiao Lin; Judith Baudet; Tianning Diao
Journal:  Angew Chem Int Ed Engl       Date:  2019-02-11       Impact factor: 15.336

7.  Iterative protecting group-free cross-coupling leading to chiral multiply arylated structures.

Authors:  Cathleen M Crudden; Christopher Ziebenhaus; Jason P G Rygus; Kazem Ghozati; Phillip J Unsworth; Masakazu Nambo; Samantha Voth; Marieke Hutchinson; Veronique S Laberge; Yuuki Maekawa; Daisuke Imao
Journal:  Nat Commun       Date:  2016-04-04       Impact factor: 14.919

  7 in total

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