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Biaryl diacid inhibitors of human s-PLA2 with anti-inflammatory activity.

Abstract：

:Twenty-four hydrophobic dicarboxylic acids are described which were evaluated as inhibitors of 14 kDa human platelet phospholipase A2 (HP-PLA2). In general, biarylacetic acid derivatives were found to be more active than biaryl acids or biarylpropanoic acids. More potent inhibitors were obtained when hydrophobic groups were attached to the biaryl acid nucleus using an olefin linkage as compared to an ether linkage. Compounds with larger hydrophobic groups were usually more potent inhibitors of HP-PLA2. Five of the compounds disclosed in this report (2, 4, 28, 36b and 36i) were found to possess significant anti-inflammatory activity in a phorbol ester induced mouse ear edema model of chronic inflammation.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Springer DM,Luh BY,Bronson JJ,McElhone KE,Mansuri MM,Gregor KR,Nettleton DO,Stanley PL,Tramposch KM

doi

10.1016/s0968-0896(00)00047-x

subject

Has Abstract

pub_date

2000-05-01 00:00:00

pages

1087-109

issue

5

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(00)00047-X

journal_volume

8

pub_type

杂志文章

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