140660-38-4Relevant academic research and scientific papers
Leukotriene B4 Receptor Antagonists: The LY255283 Series of Hydroxyacetophenones
Herron, David K.,Goodson, Theodore,Bollinger, Nancy G.,Swanson-Bean, Dorothy,Wright, Ian G.,et al.
, p. 1818 - 1828 (1992)
A series of hydroxyacetophenones was prepared for evaluation as leukotriene B4 (LTB4) receptor antagonists, culminating in 1-oxy>phenyl>ethanone (compound 35, LY255283).Using an assay for inhibition of specific LTB4 binding to human PMN, we found that substitution of a nonpolar substituent in the 5-position was required for activity.Best activity was realized with hydrogen in the 3-position, hydroxyl in the 2-position, short chain alkyl ketone in the 1-position, and a six- or eight-carbon chain linking the oxygen in the 4-position with an unsaturated terminal function.Compound 35, having an IC50 of 87 nM in the binding assay, was chosen for further preclinical evaluation.
