Rhodanine derivatives as novel inhibitors of PDE4.

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Irvine MW, Patrick GL, Kewney J, Hastings SF, MacKenzie SJ

Rhodanine derivatives as novel inhibitors of PDE4.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2032-7. doi: 10.1016/j.bmcl.2008.01.117. Epub 2008 Feb 2.

PubMed ID

18304812 [ View in PubMed

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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 (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).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
(R)-Rolipram	cAMP-specific 3',5'-cyclic phosphodiesterase 4B	IC 50 (nM)	2000	N/A	N/A	Details