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5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)—A potent FLAP inhibitor suitable for topical administration

Dermal application of the potent FLAP inhibitor, 6 (AM643) using a prototypical vehicle in a murine ear arachidonic acid model showed significant reduction in the concentrations of leukotrienes in mouse skin with concomitant reduction in ear swelling. AM643 (compound 6, 3-{3-tert-butylsulfanyl-1-[4-...

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Published in:Bioorganic & medicinal chemistry letters 2010-08, Vol.20 (15), p.4598-4601
Main Authors: Stock, Nicholas, Baccei, Christopher, Bain, Gretchen, Chapman, Charles, Correa, Lucia, Darlington, Janice, King, Christopher, Lee, Catherine, Lorrain, Daniel S., Prodanovich, Pat, Santini, Angelina, Schaab, Kevin, Evans, Jilly F., Hutchinson, John H., Prasit, Peppi
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Language:English
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Summary:Dermal application of the potent FLAP inhibitor, 6 (AM643) using a prototypical vehicle in a murine ear arachidonic acid model showed significant reduction in the concentrations of leukotrienes in mouse skin with concomitant reduction in ear swelling. AM643 (compound 6, 3-{3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid) was identified as a potential candidate for formulation as a topical agent for the treatment of skin disorders involving leukotriene production. Dermal application of 6 using a prototypical vehicle in a murine ear arachidonic acid model showed significant reduction in the concentrations of leukotrienes in mouse skin with concomitant reduction in ear swelling.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.06.011