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  • Title: A new class of leukotriene biosynthesis inhibitor: the development of MK-0591.
    Author: Prasit P, Belley M, Blouin M, Brideau C, Chan C, Charleson S, Evans JF, Frenette R, Gauthier JY, Guay J.
    Journal: J Lipid Mediat; 1993; 6(1-3):239-44. PubMed ID: 8357985.
    Abstract:
    The evolution of MK-0591 (3-[1-(4-chlorobenzyl)-3-(t-butylthio)-5-(quinolin-2-ylmethoxy+ ++)indol-2-yl]- 2,2-dimethylpropanoic acid), 12, a potent, orally active leukotriene biosynthesis inhibitor is described. MK-0591 is currently undergoing clinical evaluation as a potential agent for the treatment of asthma and inflammatory bowel disease. It acts through a novel mechanism by a specific interaction with a membrane protein, 5-lipoxygenase activating protein (FLAP), which has been shown to be essential for LT synthesis in inflammatory cells. A brief comparison of its biological activity with that of its progenitors MK-886 and L-674,636 is described.
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