Departamento de Química Orgánica, Facultad de Química, Universidad de Alcalá, Campus Universitario, 28871-Alcalá de Henares, Madrid, Spain.
Eur J Med Chem. 2012 Apr;50:90-101. doi: 10.1016/j.ejmech.2012.01.043. Epub 2012 Jan 30.
We report new examples of a series of losartan-hydrocaffeic hybrids that bear novel ester, amide and amine linkers. These compounds were made by linking hydrocaffeic acid to the side chain of losartan at the C-5 position of the imidazole ring through different strategies. Experiments performed in cultured cells demonstrate that these new hybrids retain the ability to block the angiotensin II effect and have increased antioxidant ability. Most of them reduced arterial pressure in rats better or as much as losartan.
我们报告了一系列洛沙坦-咖啡酸杂合体的新实例,这些杂合体具有新型酯、酰胺和胺连接物。这些化合物是通过不同的策略将咖啡酸连接到洛沙坦咪唑环的 C-5 位的侧链上制成的。在培养细胞中进行的实验表明,这些新的杂合体保留了阻断血管紧张素 II 作用的能力,并且抗氧化能力增强。它们中的大多数在降低大鼠血压方面的效果优于或与洛沙坦相当。