Literature DB >> 12086476

Novel 2-oxoamide inhibitors of human group IVA phospholipase A(2).

George Kokotos1, Stavroula Kotsovolou, David A Six, Violetta Constantinou-Kokotou, Christopher C Beltzner, Edward A Dennis.   

Abstract

A novel class of potent human cytosolic phospholipase A(2) (GIVA PLA(2)) inhibitors was developed. These inhibitors were designed to contain the 2-oxoamide functionality and a free carboxyl group. Among the compounds tested, a long-chain 2-oxoamide containing L-gamma-norleucine was the most potent inhibitor, causing a 50% decrease in GIVA PLA(2) activity at 0.009 mole fraction.

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Year:  2002        PMID： 12086476     DOI： 10.1021/jm025538p

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  22 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.  Differential inhibition of group IVA and group VIA phospholipases A2 by 2-oxoamides.

Authors:  Daren Stephens; Efrosini Barbayianni; Violetta Constantinou-Kokotou; Anna Peristeraki; David A Six; Jennifer Cooper; Richard Harkewicz; Raymond A Deems; Edward A Dennis; George Kokotos
Journal:  J Med Chem       Date:  2006-05-04       Impact factor: 7.446

3.  Potent and selective fluoroketone inhibitors of group VIA calcium-independent phospholipase A2.

Authors:  George Kokotos; Yuan-Hao Hsu; John E Burke; Constantinos Baskakis; Christoforos G Kokotos; Victoria Magrioti; Edward A Dennis
Journal:  J Med Chem       Date:  2010-05-13       Impact factor: 7.446

4.  Phospholipase A2 superfamily members play divergent roles after spinal cord injury.

Authors:  Rubèn López-Vales; Nader Ghasemlou; Adriana Redensek; Bradley J Kerr; Efrosini Barbayianni; Georgia Antonopoulou; Constantinos Baskakis; Khizr I Rathore; Violetta Constantinou-Kokotou; Daren Stephens; Takao Shimizu; Edward A Dennis; George Kokotos; Samuel David
Journal:  FASEB J       Date:  2011-08-25       Impact factor: 5.191

5.  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

6.  A novel monoacylglycerol lipase inhibitor with analgesic and anti-inflammatory activity.

Authors:  Victoria Magrioti; George Naxakis; Dimitra Hadjipavlou-Litina; Alexandros Makriyannis; George Kokotos
Journal:  Bioorg Med Chem Lett       Date:  2008-09-12       Impact factor: 2.823

7.  Structure-activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A(2) enzymes.

Authors:  Georgia Antonopoulou; Efrosini Barbayianni; Victoria Magrioti; Naomi Cotton; Daren Stephens; Violetta Constantinou-Kokotou; Edward A Dennis; George Kokotos
Journal:  Bioorg Med Chem       Date:  2008-11-01       Impact factor: 3.641

8.  2-Oxoamide inhibitors of phospholipase A2 activity and cellular arachidonate release based on dipeptides and pseudodipeptides.

Authors:  Efrosini Barbayianni; Daren Stephens; Andrej Grkovich; Victoria Magrioti; Yuan-Hao Hsu; Panagiotis Dolatzas; Dimitrios Kalogiannidis; Edward A Dennis; George Kokotos
Journal:  Bioorg Med Chem       Date:  2009-05-03       Impact factor: 3.641

9.  Synthesis of polyfluoro ketones for selective inhibition of human phospholipase A2 enzymes.

Authors:  Constantinos Baskakis; Victoria Magrioti; Naomi Cotton; Daren Stephens; Violetta Constantinou-Kokotou; Edward A Dennis; George Kokotos
Journal:  J Med Chem       Date:  2008-12-25       Impact factor: 7.446

10.  Differing roles for members of the phospholipase A2 superfamily in experimental autoimmune encephalomyelitis.

Authors:  Athena Kalyvas; Constantinos Baskakis; Victoria Magrioti; Violetta Constantinou-Kokotou; Daren Stephens; Rubèn López-Vales; Jian-Qiang Lu; V Wee Yong; Edward A Dennis; George Kokotos; Samuel David
Journal:  Brain       Date:  2009-02-13       Impact factor: 13.501
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