发展 N-取代羟胺作为有效的亚硝酰基（HNO）供体。
Development of N-substituted hydroxylamines as efficient nitroxyl (HNO) donors.
机构信息
Department of Chemistry, 3400 North Charles Street, Johns Hopkins University, Baltimore, Maryland 21218, USA.
出版信息
J Am Chem Soc. 2012 Feb 1;134(4):1962-5. doi: 10.1021/ja2103923. Epub 2012 Jan 17.
Due to its inherent reactivity, nitroxyl (HNO), must be generated in situ through the use of donor compounds, but very few physiologically useful HNO donors exist. Novel N-substituted hydroxylamines with carbon-based leaving groups have been synthesized, and their structures confirmed by X-ray crystallography. These compounds generate HNO under nonenzymatic, physiological conditions, with the rate and amount of HNO released being dependent mainly on the nature of the leaving group. A barbituric acid and a pyrazolone derivative have been developed as efficient HNO donors with half-lives at pH 7.4, 37 °C of 0.7 and 9.5 min, respectively.
由于其固有的反应性，亚硝酰（HNO）必须通过使用供体化合物原位生成，但目前存在的具有生理作用的 HNO 供体非常少。已经合成了具有碳离去基团的新型 N-取代羟胺，并通过 X 射线晶体学确认了它们的结构。这些化合物在非酶、生理条件下生成 HNO，HNO 的释放速率和量主要取决于离去基团的性质。已经开发出巴比妥酸和吡唑啉酮衍生物作为有效的 HNO 供体，它们在 pH 7.4、37°C 时的半衰期分别为 0.7 和 9.5 分钟。
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