Four compounds bearing amidoxime functions were synthetized: (1) 2a,b bearing an aromatic amidoxime function, (2) 2c bearing an aliphatic amidoxime function, and (3) 2d bearing aromatic and aliphatic amidoximes functions. The ability of these compounds to release NO was evaluated in vitro using the oxidative metabolism of cytochrome P450 from rat liver microsomes. Results obtained demonstrate that all amidoximes were able to release NO with a highest amount of NO produced by the 2a aromatic amidoxime. Moreover, all amidoximes exhibit cytocompatibility with human aorta smooth muscle cells. Using intracellular S-nitrosothiol formation as a marker of NO bioavailability, compounds 2a–c were demonstrated to deliver a higher amount of NO in the intracellular environment than the reference. Considering that the concentration of the bis-amidoxime 2d was two times lower that than of 2a and 2b, we can assume that 2d is the most potent molecule among the tested compounds for NO release.

合成了具有氨基a肟功能的四种化合物：（1）具有芳族氨基肟功能的2a，b，（2）具有脂肪族氨基肟功能的2c和（3）具有芳族和脂肪族氨基肟功能的2d。使用大鼠肝微粒体中细胞色素P450的氧化代谢，在体外评估了这些化合物释放NO的能力。获得的结果表明，所有a胺肟都能够释放NO，而2a芳族ox胺肟产生的NO量最高。而且，所有a胺肟都表现出与人主动脉平滑肌细胞的细胞相容性。使用细胞内S-亚硝基硫醇的形成作为NO生物利用度的标志物，化合物2a–c被证明在细胞内环境中比参照物提供更高的NO含量。考虑到双-胺肟2d的浓度比2a和2b低2倍，我们可以假定2d是被测化合物中最有效的NO释放分子。