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ID: ALA1139777

Journal: Bioorg Med Chem Lett

Title: Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.

Authors: Kuang R, Shue HJ, Blythin DJ, Shih NY, Gu D, Chen X, Schwerdt J, Lin L, Ting PC, Zhu X, Aslanian R, Piwinski JJ, Xiao L, Prelusky D, Wu P, Zhang J, Zhang X, Celly CS, Minnicozzi M, Billah M, Wang P.

Abstract: Substituted quinolyl oxazoles were discovered as a novel and highly potent series of phosphodiesterase 4 (PDE4) inhibitors. Structure-activity relationship studies revealed that the oxazole core, with 4-carboxamide and 5-aminomethyl groups, is a novel PDE4 inhibitory pharmacophore. Selectivity profiles and in vivo biological activity are also reported.

CiteXplore: 17683932

DOI: 10.1016/j.bmcl.2007.06.092