کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1392985 | 1501167 | 2012 | 9 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Novel inhibitors of nitric oxide synthase with antioxidant properties Novel inhibitors of nitric oxide synthase with antioxidant properties](/preview/png/1392985.png)
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.
A series of new mono or bicyclic nitrogen-containing heterocycles linked to an arylethanone chain were prepared and evaluated for their inhibitory potency vs nNOS and eNOS. Selected compounds were also tested to assay their antioxidant properties.Figure optionsDownload as PowerPoint slideHighlights
► New mono or bicyclic nitrogen-containing heterocycles linked to an arylethanone chain were synthesized.
► Inhibitory potency vs nNOS and eNOS in the low micromolar range was obtained.
► Selected compounds were tested to assay their antioxidant properties.
► Some compounds emerged for the combination of nNOS inhibition and antioxidant activity in the same molecule.
Journal: European Journal of Medicinal Chemistry - Volume 49, March 2012, Pages 118–126