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Volumn 8, Issue 5, 2000, Pages 1087-1109

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

Author keywords

[No Author keywords available]

Indexed keywords

2 (5,6,7,8 TETRAHYDRO 5,5,8,8 TETRAMETHYL 2 NAPHTHALENYL)METHOXY [1,1' BIPHENYL] 6,3' DICARBOXYLIC ACID; 2 [(3,4 BISPENTYLOXY)PHENYL]METHOXY 3' CARBOXY [1,1' BIPHENYL] 6 ACETIC ACID; 3' CARBOXY 2 [(1,2,3,4 TETRAHYDRO 1,1,4,4 TETRAMETHYL) 7 ANTHRACENYL] [1,1' BIPHENYL] 6 ACETIC ACID; 3' CARBOXY 2 [(5,6,7,8 TETRAHYDRO 5,5,8,8 TETRAMETHYL 2 NAPHTHALENYL) 1 PROPENYL] [1,1' BIPHENYL] 6 ACETIC ACID; 3' CARBOXY 2 [4 DECYLOXYPHENYL]METHOXY [1,1' BIPHENYL] 6 ACETIC ACID; 4 (3 CARBOXYPHENYL) 3,7 DIMETHYL 9 (2,6,6 TRIMETHYL 1 CYCLOHEXENYL) 2,4,6,8 NONATETRAENOIC ACID; ACETOACETIC ACID DERIVATIVE; DICARBOXYLIC ACID DERIVATIVE; LONAPALENE; PHOSPHOLIPASE A2 INHIBITOR; PROPIONIC ACID DERIVATIVE; UNCLASSIFIED DRUG;

EID: 0034044940     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0968-0896(00)00047-X     Document Type: Article
Times cited : (15)

References (71)
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    • 2BBr resulted in the loss of the olefin, with retention of the methoxy group. (It is possible that intramolecular Friedel-Crafts cyclization of the unsaturated ester occurred to give products containing a fluorene nucleus, but this has not been rigorously determined.).
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    • note
    • The compounds tested in the chronic inflammation in vivo assay (2, 4, 28, 36b, 36i) were not evaluated as potential inhibitors of MPO in a control experiment. Thus, the possibility exists that some (or all) of the in vivo activity reported for these compounds in the tables is a consequence of direct inhibition of the enzyme marker MPO rather than a reflection of reduced influx of neutrophils (PMNs). However, animals treated with compound 28 had significant, dose-dependent ear weight reductions that paralleled the measured reduction of myeloperoxidase activity. This implies that the drug is reducing general hyperplasia (and inflammation), and that it is not acting simply as a MPO inhibitor. Many other structurally similar (but non-biaryl) compounds were evaluated in the chronic assay for both ear weight reduction and inhibition of MPO activity. The compounds tested almost always displayed ear weight reductions that paralleled the measured reduction of myeloperoxidase activity.
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    • note
    • 2), although other explanations are possible.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.