Synthesis and evaluation of a novel series of pyrrolizine derivatives as dual cyclooxygenase-1 and 5-lipoxygenase inhibitors

被引：32

作者：

Laufer, S ^{[1
]}

Striegel, HG ^{[1
]}

Neher, K ^{[1
]}

Zechmeister, P ^{[1
]}

Donat, C ^{[1
]}

Stolingwa, K ^{[1
]}

Baur, S ^{[1
]}

Tries, S ^{[1
]}

Kammermeier, T ^{[1
]}

Dannhardt, G ^{[1
]}

Kiefer, W ^{[1
]}

机构：

[1] UNIV MAINZ,INST PHARM,D-55099 MAINZ,GERMANY

来源：

ARCHIV DER PHARMAZIE | 1997年 / 330卷 / 9-10期

关键词：

heteroarylpyrrolizines; NSAIDs; non-steroidal antiinflammatory drugs; COX-1; cyclooxygenase-1; 5-LOX; 5-lipoxygenase; ELISA; enzyme linked immunosorbent assay;

D O I：

10.1002/ardp.19973300908

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The aim of our study was to investigate structure activity relationship following the replacement of the B-phenyl substituent at the 6,7-diaryl-2,3-dihydropyrrolizine template by various heteroaromatic residues. In this context we developed a new, efficient, and highly sensitive test method for the screening of dual cyclooxygenase-l (COX-1) and 5-lipoxygenase (5-LOX) inhibitors. We used human platelets as a source of COX-1 and human PMNLs as a source of 5-LOX. Both cell types were isolated from the same volume of blood. PGE(2) and LTB4 respectively were determined by highly selective and sensitive ELISA kits, using monoclonal antibodies. For a single determination at most 0.5 mt whole blood is needed.

引用

页码：307 / 312

页数：6

共 30 条

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