O-alkylcarboxylate oxime and N-hydroxyurea analogs of substituted indole leukotriene biosynthesis inhibitors

…, RG Maki, KE Rodriques, JB Bouska, P Young…

Index: Woods, Keith W.; Brooks, Clint D. W.; Maki, Robert G.; Rodriques, Karen E.; Bouska, Jennifer B.; Young, Patrick; Bell, Randy L.; Carter, George W. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 13 p. 1547 - 1552

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Citation Number: 18

Abstract

Reference FLAP inhibitors 1 and 2 were converted into the corresponding O-acetic acid oxime congeners 8 and 11a, respectively, resulting in potent, orally active, leukotriene biosynthesis inhibitors. An attempt to create a dual FLAP and direct 5-LO inhibitor by replacing the carboxylate group in 1 with the N-hydroxyurea pharmacophore did not provide superior inhibitors.