Argüello J, Núñez-Vergara L J, Bollo S, Squella J A
Bioelectrochemistry Laboratory, Chemical and Pharmaceutical Sciences Faculty, University of Chile, POB 233, Santiago 1, Chile.
Bioelectrochemistry. 2006 Sep;69(1):104-12. doi: 10.1016/j.bioelechem.2005.12.003. Epub 2006 Feb 13.
Three new nitrofuryl substituted 1,4-dihydropyridine derivatives were electrochemically tested in the scope of newly found compounds useful as chemotherapeutic alternative to the Chagas' disease. All the compounds were capable to produce nitro radical anions sufficiently stabilized in the time window of the cyclic voltammetric experiment. In order to quantify the stability of the nitro radical anion we have calculated the decay constant, k2. Furthermore, from the voltammetric results, some parameters of biological significance as E7(1) (indicative of in vivo nitro radical anion formation) and KO2 (thermodynamic indicator of oxygen redox cycling) have been calculated. From the comparison of E7(1), KO2 and k2 values between the studied nitrofuryl 1,4-DHP derivatives and well-known current drugs an auspicious activity for one of the studied compounds i.e. FDHP2, can be expected.
在新发现的可用作恰加斯病化疗替代物的化合物范围内，对三种新的硝基呋喃取代的1,4 - 二氢吡啶衍生物进行了电化学测试。所有化合物都能够产生在循环伏安实验时间窗口内充分稳定的硝基自由基阴离子。为了量化硝基自由基阴离子的稳定性，我们计算了衰减常数k2。此外，根据伏安法结果，还计算了一些具有生物学意义的参数，如E7(1)（指示体内硝基自由基阴离子形成）和KO2（氧氧化还原循环的热力学指标）。通过比较所研究的硝基呋喃基1,4 - DHP衍生物与知名现有药物之间的E7(1)、KO2和k2值，可以预期其中一种所研究的化合物即FDHP2具有良好的活性。
