Rhodanine derivatives as novel inhibitors of PDE4

Mark W. Irvine, Graham L. Patrick, Justin Kewney, Stuart F. Hastings, Simon J. MacKenzie

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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 ( IC50 = 0.89 & 0.74 mu M). The replacement of rhodanine with structurally related heterocycles was also investigated and led to the synthesis of pseudothiohydantoin 7 ( IC50 = 0.31 mu M).
Original languageEnglish
Pages (from-to)2032-2037
JournalBioorganic & Medicinal Chemistry Letters
Volume18
Issue number6
DOIs
Publication statusPublished - 15 Mar 2008

Cite this

Irvine, M. W., Patrick, G. L., Kewney, J., Hastings, S. F., & MacKenzie, S. J. (2008). Rhodanine derivatives as novel inhibitors of PDE4. Bioorganic & Medicinal Chemistry Letters, 18(6), 2032-2037. https://doi.org/10.1016/j.bmcl.2008.01.117