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Bioorg Med Chem Lett. 2012 Jan 15;22(2):1237-41. doi: 10.1016/j.bmcl.2011.11.073. Epub 2011 Nov 25.

Heteroaromatic-aminomethyl quinolones: potent and selective iNOS inhibitors.

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  • 1Afraxis, La Jolla, CA 92037, United States.

Abstract

The overproduction of nitric oxide during the biological response to inflammation by the nitric oxide synthase (NOS) enzymes have been implicated in the pathology of many diseases. By removal of the amide core from uHTS-derived quinolone 4, a new series highly potent heteroaromatic-aminomethyl quinolone iNOS inhibitors 8 were identified. SAR studies led to identification of piperazine 22 and pyrimidine 32, both of which reduced plasma nitrates following oral dosing in a mouse lipopolysaccharide challenge assay.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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