Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 9, Pages 2821-2828Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm050993h
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Funding
- NIGMS NIH HHS [R01 GM064611-05A2S1, GM 064611, R01 GM020501, GM 20501, R01 GM020501-32, R01 GM064611, F32 GM020501] Funding Source: Medline
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Inhibitors of the Group IVA phospholipase A(2) (GIVA cPLA(2)) and GVIA iPLA(2) are useful tools for defining the roles of these enzymes in cellular signaling and inflammation. We have developed inhibitors of GVIA iPLA(2) building upon the 2-oxoamide backbone that are uncharged, containing ester groups. Although the most potent inhibitors of GVIA iPLA(2) also inhibited GIVA cPLA(2), there were three 2-oxoamide compounds that selectively and weakly inhibited GVIA iPLA(2). We further show that several potent 2-oxoamide inhibitors of GIVA cPLA(2) containing free carboxylic groups (Kokotos et al. J. Med. Chem. 2002, 45, 2891-2893) do not inhibit GVIA iPLA(2) and are, therefore, selective GIVA cPLA(2) inhibitors.
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