Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.
Article Details
- CitationCopy to clipboard
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]
- 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
Drug Target Property Measurement pH Temperature (°C) Ibuprofen Prostaglandin G/H synthase 2 IC 50 (nM) 100 N/A N/A Details Indomethacin Prostaglandin G/H synthase 2 IC 50 (nM) 560 N/A N/A Details Naproxen Prostaglandin G/H synthase 2 IC 50 (nM) 2500 N/A N/A Details Zileuton Arachidonate 5-lipoxygenase IC 50 (nM) 760 N/A N/A Details