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Nicotinamide N-oxide研究進展

發(fā)布日期：2017-10-30   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/Nicotinamide_N-oxide.htmlNicotinamide N-oxide/a產(chǎn)品描述：Nicotinamide N-oxide, an
<a href="https://www.medchemexpress.com/Nicotinamide_N-oxide.html">Nicotinamide N-oxide</a>產(chǎn)品描述：Nicotinamide N-oxide, an <i>in vivo</i> nicotinamide metabolite, is a potent, and selective antagonist of the <b>CXCR2</b> receptor.

<i><b>In Vitro:</b></i> Nicotinamide is one of the forms of vitamin B<sub>3</sub>. It is a precursor for nicotinamide adenine dinucleotide, which is best known as an electron carrier in oxidative phosphorylation and as a cofactor for many dehydrogenases. It is metabolized through two enzymatic systems. The first system starts with the methylation of nicotinamide by nicotinamide N-methyltransferase, which can subsequently be oxidized by aldehyde oxidase. The second enzymatic system oxidizes nicotinamide to nicotinamide N-oxide<sup>[1]</sup>. A series of nicotinamide N-oxides is synthesized and shown to be novel, potent, and selective antagonists of the CXCR2 receptor. Compound 1 has demonstrated potent inhibition of neutrophil chemotaxis (IC<sub>50</sub>=10 nM). Compound 2 is a selective antagonist of IL-8 binding (IC<sub>50</sub>=110 nM) and potent inh<br><br>
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