117423-74-2

Upstream product

• 123-11-5 4-methoxy-benzaldehyde 
• 117424-79-0 ethyl 5-<3-(ethoxycarbonyl)benzoyl>-2-methoxybenzenepropanoate 
• 128578-16-5 5-[[3-(ethoxycarbonyl)phenyl]carbonyl]-2-hydroxybenzenepropanoic acid ethyl ester 
• 117424-80-3 5-(3-carboxybenzoyl)-2-hydroxybenzenepropanoic acid 
• 134578-03-3 (E)-6-(4-methoxyphenyl)-5-hexenyl methanesulfonate 
• 81077-29-4 (E)-6-(4-methoxyphenyl)pent-5-enoic acid 
• 17814-85-6 (4-carboxybutyl)triphenylphosphonium bromide 
• 70311-27-2 2-methoxybenzenepropanoic acid ethyl ester 
• 67326-20-9 3-carbethoxybenzoyl chloride 
• 128577-60-6 (5E)-6-(4-Methoxyphenyl)-5-hexen-1-ol 
• 128577-80-0 3-{3-(2-Ethoxycarbonyl-ethyl)-4-[(E)-6-(4-methoxy-phenyl)-hex-5-enyloxy]-benzoyl}-benzoic acid ethyl ester 

Relevant academic research and scientific papers

Intermediates for leukotriene antagonists

This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.

Benzophenone Dicarboxylic Acid Antagonists of Leukotriene B4. 2. Structure-Activity Relationships of the Lipophilic Side Chain

A series of lipophilic benzophenone dicarboxylic acid derivatives were found to inhibit the binding of the potent chemotoxin leukotriene B4 (LTB4) to its receptor on intact human neutrophils.Activity at the LTB4 receptor was determined by using a 3H>LTB4-binding assay.The structure-activity relationship for the lipophilic side chain was systematically investigated.Compounds with n-alkyl side chains of varying lengths were prepared and tested.Best inhibition of 3H>LTB4 binding was observed with the n-decyl derivative.Analogues with alkyl chains terminated with an aromatic ring showed improved activity.The 6-phenylhexyl side chain was optimal.Substitution on the terminal aromatic ring was also evaluated.Methoxyl, methylsulfinyl, and methyl substituents greatly enhanced the activity of the compound.For a given substituent, the para isomer had the best activity.Thus the nature of the lipophilic side chain can greatly influence the ability of the compounds to inhibit the binding of LTB4 to its receptor on intact human neutrophils.The most active compound from this series, 84 (LY223982), bound to the LTB4 receptor with the affinity approaching that of the agonist.