<?xml version="1.0" encoding="UTF-8"?><xml><records><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Six, D. A.</style></author><author><style face="normal" font="default" size="100%">Barbayianni, E.</style></author><author><style face="normal" font="default" size="100%">Loukas, V.</style></author><author><style face="normal" font="default" size="100%">Constantinou-Kokotou, V.</style></author><author><style face="normal" font="default" size="100%">Hadjipavlou-Litina, D.</style></author><author><style face="normal" font="default" size="100%">Stephens, D.</style></author><author><style face="normal" font="default" size="100%">Wong, A. C.</style></author><author><style face="normal" font="default" size="100%">Magrioti, V.</style></author><author><style face="normal" font="default" size="100%">Moutevelis-Minakakis, P.</style></author><author><style face="normal" font="default" size="100%">Baker, S. F.</style></author><author><style face="normal" font="default" size="100%">Dennis, E. A.</style></author><author><style face="normal" font="default" size="100%">Kokotos, G.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Structure-activity relationship of 2-oxoamide inhibition of group IVA cytosolic phospholipase A&lt;sub&gt;2&lt;/sub&gt; and group V secreted phospholipase A&lt;sub&gt;2&lt;/sub&gt;</style></title><secondary-title><style face="normal" font="default" size="100%">Journal of Medicinal Chemistry</style></secondary-title><alt-title><style face="normal" font="default" size="100%">J Med Chem</style></alt-title><short-title><style face="normal" font="default" size="100%">J Med ChemJ Med Chem</style></short-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">amide triacylglycerol analogs</style></keyword><keyword><style  face="normal" font="default" size="100%">amino-acids</style></keyword><keyword><style  face="normal" font="default" size="100%">arachidonic-acid</style></keyword><keyword><style  face="normal" font="default" size="100%">carboxylic-acids</style></keyword><keyword><style  face="normal" font="default" size="100%">crystal-structure</style></keyword><keyword><style  face="normal" font="default" size="100%">group iia</style></keyword><keyword><style  face="normal" font="default" size="100%">lysophospholipase activity</style></keyword><keyword><style  face="normal" font="default" size="100%">nonsteroidal antiinflammatory drugs</style></keyword><keyword><style  face="normal" font="default" size="100%">one-pot conversion</style></keyword><keyword><style  face="normal" font="default" size="100%">selective inhibitor</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2007</style></year><pub-dates><date><style  face="normal" font="default" size="100%">Aug 23</style></date></pub-dates></dates><number><style face="normal" font="default" size="100%">17</style></number><volume><style face="normal" font="default" size="100%">50</style></volume><pages><style face="normal" font="default" size="100%">4222-4235</style></pages><isbn><style face="normal" font="default" size="100%">0022-2623</style></isbn><language><style face="normal" font="default" size="100%">English</style></language><abstract><style face="normal" font="default" size="100%">&lt;span&gt;The Group IVA cytosolic phospholipase A&lt;/span&gt;&lt;sub&gt;&lt;span&gt;2&lt;/span&gt;&lt;/sub&gt;&lt;span&gt;&amp;nbsp;(GIVA cPLA&lt;/span&gt;&lt;sub&gt;&lt;span&gt;2&lt;/span&gt;&lt;/sub&gt;&lt;span&gt;) is a key provider of substrates for the production of eicosanoids and platelet-activating factor. We explored the structure−activity relationship of 2-oxoamide-based compounds and GIVA cPLA&lt;/span&gt;&lt;sub&gt;&lt;span&gt;2&lt;/span&gt;&lt;/sub&gt;&lt;span&gt;&amp;nbsp;inhibition. The most potent inhibitors are derived from δ- and γ-amino acid-based 2-oxoamides. The optimal side-chain moiety is a short nonpolar aliphatic chain. All of the newly developed 2-oxoamides as well as those previously described have now been tested with the human Group V secreted PLA&lt;/span&gt;&lt;sub&gt;&lt;span&gt;2&lt;/span&gt;&lt;/sub&gt;&lt;span&gt;&amp;nbsp;(GV sPLA&lt;/span&gt;&lt;sub&gt;&lt;span&gt;2&lt;/span&gt;&lt;/sub&gt;&lt;span&gt;) and the human Group VIA calcium-independent PLA&lt;/span&gt;&lt;sub&gt;&lt;span&gt;2&lt;/span&gt;&lt;/sub&gt;&lt;span&gt;&amp;nbsp;(GVIA iPLA&lt;/span&gt;&lt;sub&gt;&lt;span&gt;2&lt;/span&gt;&lt;/sub&gt;&lt;span&gt;). Only one 2-oxoamide compound had appreciable inhibition of GV sPLA&lt;/span&gt;&lt;sub&gt;&lt;span&gt;2&lt;/span&gt;&lt;/sub&gt;&lt;span&gt;, and none of the potent GIVA cPLA&lt;/span&gt;&lt;sub&gt;&lt;span&gt;2&lt;/span&gt;&lt;/sub&gt;&lt;span&gt;&amp;nbsp;inhibitors inhibited either GV sPLA&lt;/span&gt;&lt;sub&gt;&lt;span&gt;2&lt;/span&gt;&lt;/sub&gt;&lt;span&gt;&amp;nbsp;or GVIA iPLA&lt;/span&gt;&lt;sub&gt;&lt;span&gt;2&lt;/span&gt;&lt;/sub&gt;&lt;span&gt;. Two of these specific GIVA cPLA&lt;/span&gt;&lt;sub&gt;&lt;span&gt;2&lt;/span&gt;&lt;/sub&gt;&lt;span&gt;&amp;nbsp;inhibitors were also found to have potent therapeutic effects in animal models of pain and inflammation at dosages well below the control nonsteroidal anti-inflammatory drugs.&lt;/span&gt;</style></abstract><issue><style face="normal" font="default" size="100%">17</style></issue><accession-num><style face="normal" font="default" size="100%">ISI:000248758600026</style></accession-num><auth-address><style face="normal" font="default" size="100%">Dennis, EAUniv Calif San Diego, Sch Med, Dept Chem &amp; Biochem, MC 0601, La Jolla, CA 92093 USAUniv Calif San Diego, Sch Med, Dept Chem &amp; Biochem, MC 0601, La Jolla, CA 92093 USAUniv Calif San Diego, Sch Med, Dept Chem &amp; Biochem, La Jolla, CA 92093 USAUniv Calif San Diego, Sch Med, Dept Pharmacol, La Jolla, CA 92093 USAUniv Athens, Dept Chem, Organ Chem Lab, Athens 15771, GreeceAgr Univ Athens, Chem Labs, Athens 11855, GreeceAristotle Univ Thessaloniki, Sch Pharm, Dept Pharmaceut Chem, Thessaloniki 54124, Greece</style></auth-address></record></records></xml>