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Summary
Novelty: Substituted phenyl-(2-hydroxy)ethylpyridine compounds and their ketone and alkyl analogues are claimed in WO948880 (AG2453). Very similar compounds are claimed in AG2454 (WO9118879). AG2446 (WO9118601) claims amine, ether or thioether linked pyridyl-benzoic acids derivatives. These compounds are potentially useful for diseases attributed to hydroxyleukotrienes, especially LTB4 and LTB4 agonists.
Biology: The biological data presented in all three patents is essentially the same. Antagonist activity is demonstrated by low levels of antagonism towards agonists such as potassium chloride, carbachol, histamine and PGF2. The receptor binding affinity of the compounds is assessed on [3H]-LTB4 binding to human U937 cell membranes. LTB4 antagonist activity is measured by the ability to antagonize the LTB4 elicited calcium transient, measured with fura-2 fluorescent calcium probe.
Chemistry: The syntheses are described using reaction flow diagrams. Four compounds are specifically claimed in AG2453 including 2-(E-2-carboxyethenyl)-3-decyloxy-6-[2-(3-carboxyphenyl)-2-hydroxy]ethylpyridine, dilithium salt. 3-[1-Oxythia-2-[2-(E-2-Carboxyethenyl)-3-dodecyloxy-6-pyridyl]ethyl]-benzoic acid is claimed in AG2446 along with thirteen related compounds.
Structure: