117690-48-9

Upstream product

• 109-65-9 1-bromo-butane 
• 38987-01-8 5-allyl-2,4-dihydroxyacetophenone 
• 89-84-9 2',4'-dihydroxy-4-acetophenone 
• 117705-60-9 1-(4-allyloxy-2-methoxy-phenyl)-ethanone 
• 117705-59-6 5-allyl-4-hydroxy-2-methoxyacetophenone 
• 40815-74-5 4-allyloxy-2-hydroxyacetophenone 

Relevant academic research and scientific papers

Leukotriene B4 Receptor Antagonists: The LY255283 Series of Hydroxyacetophenones

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.

ANTI-INFLAMMATORY AGENTS

This invention provides benzene derivatives, pharmaceutical formulations of those derivatives, and a method of using the derivatives for the treatment of inflammation in mammals.