Martínez Carlos H Ríos, Dardonville Christophe
Instituto de Química Médica, IQM-CSIC , Juan de la Cierva 3, E-28006 Madrid, Spain.
ACS Med Chem Lett. 2012 Nov 20;4(1):142-5. doi: 10.1021/ml300326v. eCollection 2013 Jan 10.
We have developed a methodology that enables for the rapid measurement of ionization constants (pK a) of series of compounds by UV spectrophotometry. This protocol, which is straightforward to set up, takes advantage of the sensitivity of UV spectroscopy and the throughput enabled by the 96-well microplate (as opposed to the use of 1 cm quartz cuvette). The compounds, in stock solutions in DMSO, are dissolved in several aqueous buffer solutions directly in the microtiter plate, allowing the simultaneous determination of the UV spectra as a function of pH. Further treatment of the data provides the pK a values in a medium-throughput manner. The pK a values of 11 new antitrypanosomal dibasic compounds were determined using this methodology.
我们开发了一种方法，能够通过紫外分光光度法快速测量一系列化合物的电离常数（pKa）。该方案易于设置，利用了紫外光谱的灵敏度以及96孔微孔板实现的通量（与使用1厘米石英比色皿相反）。将二甲基亚砜储备溶液中的化合物直接溶解在微孔板中的几种水性缓冲溶液中，从而能够同时测定作为pH函数的紫外光谱。对数据的进一步处理以中等通量的方式提供pKa值。使用该方法测定了11种新型抗锥虫二元化合物的pKa值。
