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Eur J Med Chem. 2012 Mar;49:118-26. doi: 10.1016/j.ejmech.2012.01.002. Epub 2012 Jan 11.

Novel inhibitors of nitric oxide synthase with antioxidant properties.

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Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, Catania, Italy.


We previously described a series of imidazole-based inhibitors substituted at N-1 with an arylethanone chain as interesting inhibitors of neuronal nitric oxide synthase (nNOS), endowed with good selectivity vs endothelial nitric oxide synthase (eNOS). As a follow up of these studies, several analogs characterized by the presence of substituted imidazoles or other mono or bicyclic nitrogen-containing heterocycles instead of simple imidazole were synthesized, and their biological evaluation as in vitro inhibitors of both nNOS and eNOS is described herein. Most of these compounds showed improved nNOS and eNOS inhibitory activity with respect to reference inhibitors. Selected compounds were also tested to analyze their antioxidant properties. Some of them displayed good capacity to scavenge free radicals and ability to reduce lipid peroxidation.

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