作者: Spaethe, Stephen M. ; Goodson, Theodore ; Fleisch, Jerome H. ; Froelich, Larry L. ; Sofia, Michael J. ; Marder, Philip ; Roman Carlos R. ; Nelson, Katrina ; Herron, David K.

A series of 2-alkyl-4-ethyl-5-[6-methyl-6-(2H-tetrazol-5-yl)heptyloxy]phenols were prepared and shown to be potent leukotriene B₄ (LTB₄) receptor antagonists.They bound to the human neutrophil and guinea pig lung LTB₄ receptors with high affinity.Each compound was also shown to be effective at antagonizing the effects of LTB₄-induced integrin up-regulation on human neutrophils and on LTB₄-mediated contraction of guinea pig lung parenchyma.

1992-12-01·BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

-alkoxyphenol leukotriene B4 receptor antagonists: effect of a chroman carboxylic acid.

作者: Saussy, David L. Jr. ; Cockerham, Sandra L. ; Stengel, Peter W. ; Silbaugh, Steven A. ; Froelich, Larry L. ; Marder, Philip ; Sofia, Michael J. ; Jackson, William T.

Several o-alkoxyphenols containing a chroman carboxylic acid side-chain have been prepared as antagonists of leukotriene B₄ receptors.These antagonists were compared to their parent alkoxyphenols containing the tetrazole acid side-chain.These chroman containing antagonists retained their binding potency for human neutrophil receptors; however, showed enhanced potency against guinea pig receptors in both in vitro and in vivo systems.

1992-12-01·BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

-alkoxyphenol leukotriene B4 receptor antagonists

作者: Saussy, David L. Jr. ; Cockerham, Sandra L. ; Stengel, Peter W. ; Froelich, Larry L. ; Sofia, Michael j. ; Silbaugh, Steven A. ; Jackson, William T.

A series of o-alkoxyphenols containing a tetrazole acid side chain, e.g., I, have been prepared as antagonists of leukotriene B₄ receptors.These compounds were tested as receptor antagonists of human neutrophil and guinea pig lung membrane leukotriene B₄ receptors.Compounds in this series were found to be up to 18-fold more potent than LY255283.These results indicate that the acyl group of the 1,2,4,5-substituted hydroxyacetophenone class of LTB₄ antagonists is not critical to antagonist potency.

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