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Updated: May 26, 2026

Synthesis and Assay of Vibrio Quorum Sensing Inhibitors
Published on: May 31, 2024
Heteroaromatic-aminomethyl quinolones: potent and selective iNOS inhibitors
Sergio G Durón1, Andrew Lindstrom, Céline Bonnefous
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.
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