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  • Title: Synthesis of indolylalkoxyiminoalkylcarboxylates as leukotriene biosynthesis inhibitors.
    Author: Kolasa T, Bhatia P, Brooks CD, Hulkower KI, Bouska JB, Harris RR, Bell RL.
    Journal: Bioorg Med Chem; 1997 Mar; 5(3):507-14. PubMed ID: 9113329.
    Abstract:
    A series of substituted indolylalkoxyiminoalkylcarboxylates were found to be potent leukotriene biosynthesis inhibitors. The structure-activity relationships were investigated. Representative potent inhibitors identified were the quinolyl 3a (A-86885) and pyridyl 3b (A-86886) congeners with in vitro IC50s of 21 and 9 nM and in vivo leukotriene inhibition in the rat with oral ED50s of 0.9 and 1.7 mg/kg, respectively.
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