Rhodanine derivatives as novel inhibitors of PDE4

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

Research output: Contribution to journalArticlepeer-review

53 Citations (Scopus)

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

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