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 journalArticle

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
Irvine, Mark W. ; Patrick, Graham L. ; Kewney, Justin ; Hastings, Stuart F. ; MacKenzie, Simon J. / Rhodanine derivatives as novel inhibitors of PDE4. In: Bioorganic & Medicinal Chemistry Letters. 2008 ; Vol. 18, No. 6. pp. 2032-2037.
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Irvine, MW, Patrick, GL, Kewney, J, Hastings, SF & MacKenzie, SJ 2008, 'Rhodanine derivatives as novel inhibitors of PDE4' Bioorganic & Medicinal Chemistry Letters, vol. 18, no. 6, pp. 2032-2037. https://doi.org/10.1016/j.bmcl.2008.01.117

Rhodanine derivatives as novel inhibitors of PDE4. / Irvine, Mark W.; Patrick, Graham L.; Kewney, Justin; Hastings, Stuart F.; MacKenzie, Simon J.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 18, No. 6, 15.03.2008, p. 2032-2037.

Research output: Contribution to journalArticle

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Irvine MW, Patrick GL, Kewney J, Hastings SF, MacKenzie SJ. Rhodanine derivatives as novel inhibitors of PDE4. Bioorganic & Medicinal Chemistry Letters. 2008 Mar 15;18(6):2032-2037. https://doi.org/10.1016/j.bmcl.2008.01.117