Leukotriene B4 receptor antagonists: the LY255283 series of hydroxyacetophenones

…, NG Bollinger, D Swanson-Bean…

Index: Herron, David K.; Goodson, Theodore; Bollinger, Nancy G.; Swanson-Bean, Dorothy; Wright, Ian G.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 10 p. 1818 - 1828

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Citation Number: 52

Abstract

A series of hydroxyacetophenones was prepared for evaluation as leukotriene B4 (LTB4) receptor antagonieta, culminating in 1-[5-ethyl-2-hydroxy-4-[[6-methyl-6-(lH-tetrazol-5yl) heptyl] oxy] phenyl] ethanone (compound 35, LY255283). Using an assay for inhibition of specific [3H] LTB4 binding to human PMN, we found that substitution of a nonpolar substituent in the &position was required for activity. Best activity was realized with ...