Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights.

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Gradler U, Fuchss T, Ulrich WR, Boer R, Strub A, Hesslinger C, Anezo C, Diederichs K, Zaliani A

Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights.

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4228-32. doi: 10.1016/j.bmcl.2011.05.073. Epub 2011 May 30.

PubMed ID

21684157 [ View in PubMed

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Abstract

Inducible arginine oxidation and subsequent NO production by correspondent synthase (iNOS) are important cellular answers to proinflammatory signals. Prolonged NO production has been proved in higher organisms to cause stroke or septic shock. Several classes of potent NOS inhibitors have been reported, most of them targeting the arginine binding site of the oxygenase domain. Here we disclose the SAR and the rational design of potent and selective iNOS inhibitors which may be useful as anti-inflammatory drugs.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
1-(6-CYANO-3-PYRIDYLCARBONYL)-5',8'-DIFLUOROSPIRO[PIPERIDINE-4,2'(1'H)-QUINAZOLINE]-4'-AMINE	Nitric oxide synthase, inducible	IC 50 (nM)	37.15	N/A	N/A	Details