Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.

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Kolasa T, Brooks CD, Rodriques KE, Summers JB, Dellaria JF, Hulkower KI, Bouska J, Bell RL, Carter GW

Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.

J Med Chem. 1997 Feb 28;40(5):819-24.

PubMed ID
9057869 [ View in PubMed
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Abstract

Representative nonsteroidal anti-inflammatory drug (NSAID) cyclooxygenase inhibitors such as ibuprofen, naproxen, and indomethacin were used as orally bioavailable scaffolds to design selective 5-lipoxygenase (5-LO) inhibitors. Replacement of the NSAID carboxylic acid group with a N-hydroxyurea group provided congeners with selective 5-LO inhibitory activity.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
IbuprofenProstaglandin G/H synthase 2IC 50 (nM)100N/AN/ADetails
IndomethacinProstaglandin G/H synthase 2IC 50 (nM)560N/AN/ADetails
NaproxenProstaglandin G/H synthase 2IC 50 (nM)2500N/AN/ADetails
ZileutonArachidonate 5-lipoxygenaseIC 50 (nM)760N/AN/ADetails