Rhodanine derivatives as novel inhibitors of PDE4

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

doi:10.1016/j.bmcl.2008.01.117

Rhodanine derivatives as novel inhibitors of PDE4

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

School of Health and Life Sciences

Research output: Contribution to journal › Article › peer-review

54 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 language	English
Pages (from-to)	2032-2037
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	18
Issue number	6
DOIs	https://doi.org/10.1016/j.bmcl.2008.01.117
Publication status	Published - 15 Mar 2008

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10.1016/j.bmcl.2008.01.117

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title = "Rhodanine derivatives as novel inhibitors of PDE4",

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). ",

author = "Irvine, {Mark W.} and Patrick, {Graham L.} and Justin Kewney and Hastings, {Stuart F.} and MacKenzie, {Simon J.}",

year = "2008",

month = mar,

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doi = "10.1016/j.bmcl.2008.01.117",

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journal = "Bioorganic & Medicinal Chemistry Letters",

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T1 - Rhodanine derivatives as novel inhibitors of PDE4

AU - Irvine, Mark W.

AU - Patrick, Graham L.

AU - Kewney, Justin

AU - Hastings, Stuart F.

AU - MacKenzie, Simon J.

PY - 2008/3/15

Y1 - 2008/3/15

N2 - 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).

AB - 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).

U2 - 10.1016/j.bmcl.2008.01.117

DO - 10.1016/j.bmcl.2008.01.117

M3 - Article

SN - 0960-894X

VL - 18

SP - 2032

EP - 2037

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 6

ER -

Rhodanine derivatives as novel inhibitors of PDE4

Abstract

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