Literature DB >> 15203135

Synthesis and evaluation of substrate-mimicking cytosolic phospholipase A2 inhibitors--reducing the lipophilicity of the arachidonyl chain isostere.

Iain Walters1, Colin Bennion, Stephen Connolly, Pamela J Croshaw, Kim Hardy, Paul Hartopp, Clive G Jackson, Sarah J King, Louise Lawrence, Antonio Mete, David Murray, David H Robinson, Linda Stein, Edward Wells, W John Withnall.   

Abstract

The high lipophilicity of a series of cytosolic phospholipase A(2) inhibitors has been reduced by the modification of a decyloxyphenyl chain designed to mimic the arachidonyl group of the natural substrate. These changes have resulted in an improvement in the whole cell potency of the inhibitors.

Entities:  

Mesh:

Substances:

Year:  2004        PMID: 15203135     DOI: 10.1016/j.bmcl.2004.05.024

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


  3 in total

Review 1.  Phospholipase A2 enzymes: physical structure, biological function, disease implication, chemical inhibition, and therapeutic intervention.

Authors:  Edward A Dennis; Jian Cao; Yuan-Hao Hsu; Victoria Magrioti; George Kokotos
Journal:  Chem Rev       Date:  2011-09-12       Impact factor: 60.622

2.  2-Oxoamide inhibitors of cytosolic group IVA phospholipase A2 with reduced lipophilicity.

Authors:  Georgia Antonopoulou; Victoria Magrioti; Maroula G Kokotou; Aikaterini Nikolaou; Efrosini Barbayianni; Varnavas D Mouchlis; Edward A Dennis; George Kokotos
Journal:  Bioorg Med Chem       Date:  2016-07-27       Impact factor: 3.641

3.  Pharmacophore-based discovery of a novel cytosolic phospholipase A(2)α inhibitor.

Authors:  Stefan M Noha; Bianca Jazzar; Susanne Kuehnl; Judith M Rollinger; Hermann Stuppner; Anja M Schaible; Oliver Werz; Gerhard Wolber; Daniela Schuster
Journal:  Bioorg Med Chem Lett       Date:  2011-11-30       Impact factor: 2.823

  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.