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ID: ALA1142363

Journal: Bioorg Med Chem Lett

Title: Rhodanine derivatives as novel inhibitors of PDE4.

Authors: Irvine MW, Patrick GL, Kewney J, Hastings SF, MacKenzie SJ.

Abstract: The discovery, synthesis and in vitro activity of a novel series of rhodanine based phosphodiesterase-4 (PDE4) inhibitors is described. Structure-activity relationship studies directed toward improving potency led to the development of submicromolar inhibitors 2n and 3i (IC(50)=0.89 & 0.74 microM). The replacement of rhodanine with structurally related heterocycles was also investigated and led to the synthesis of pseudothiohydantoin 7 (IC(50)=0.31 microM).

CiteXplore: 18304812

DOI: 10.1016/j.bmcl.2008.01.117