The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS).

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Cheshire DR, Aberg A, Andersson GM, Andrews G, Beaton HG, Birkinshaw TN, Boughton-Smith N, Connolly S, Cook TR, Cooper A, Cooper SL, Cox D, Dixon J, Gensmantel N, Hamley PJ, Harrison R, Hartopp P, Kack H, Leeson PD, Luker T, Mete A, Millichip I, Nicholls DJ, Pimm AD, St-Gallay SA, Wallace AV

The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS).

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2468-71. doi: 10.1016/j.bmcl.2011.02.061. Epub 2011 Feb 18.

PubMed ID

21398123 [ View in PubMed

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Abstract

By careful analysis of experimental X-ray ligand crystallographic protein data across several inhibitor series we have discovered a novel, potent and selective series of iNOS inhibitors exemplified by compound 8.

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)	1000	N/A	N/A	Details
1-(6-CYANO-3-PYRIDYLCARBONYL)-5',8'-DIFLUOROSPIRO[PIPERIDINE-4,2'(1'H)-QUINAZOLINE]-4'-AMINE	Nitric oxide synthase, inducible	IC 50 (nM)	41	N/A	N/A	Details