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Anti-Inflammatory, Anti-Allergic, Respiratory & GI Agents

Anti-Allergic/Leukotriene Antagonists: Novel Benzophenone Derivatives as Potent Leukotriene Antagonists

Pages 637-638 | Published online: 02 Mar 2011
 

Summary

Novelty: The treatment of allergic disorders using leukotriene (LT) antagonists derived from novel diaryl ketones, diaryl ethers etc is claimed.

Biology: Assays showing in vitro LTD4 receptor antagonism are described. The compound below shows 87% inhibition of LTB4-induced aggregation at 10−6 M and 92% inhibition of LTB4-binding (human neutrophils) at 10−7 M.

Chemistry: There are one hundred and five synthetic examples though many are described by analogy. The illustrated compound is 5-(3-carboxybenzoyl)-2-(6-(4-methoxyphenyl)-5-hexenyl)oxy-benzenepropionic acid.

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