Department of Analytical Chemistry, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Medical University of Silesia in Katowice, PL-4 Jagiellońska Street, 41-200 Sosnowiec, Poland.
Molecules. 2019 Sep 2;24(17):3187. doi: 10.3390/molecules24173187.
The aim of this study was to assess the lipophilicity of selected antiparasitic, antihypertensive and non-steroidal anti-inflammatory drugs (NSAIDs) by means of reversed phase-thin layer chromatography (RP-TLC) as well by using Soczewiński-Wachtmeister's and J. Ościk's equations. The lipophilicity parameters of all examined compounds obtained under various chromatographic systems (i.e., methanol-water and acetone-water, respectively) and those determined on the basis of Soczewiński-Wachtmeister's and Ościk's equations (i.e., R and R) were compared with the theoretical ones (e.g., AlogPs, AClogP, milogP, AlogP, MlogP, XlogP2, XlogP3) and the experimental value of the partition coefficient (logP). It was found that the R parameter may be a good alternative tool in describing the lipophilic nature of biologically active compounds with a high and low lipophilicity (i.e., antihypertensive and antiparasitic drugs). Meanwhile, the R was more suitable for compounds with a medium lipophilicity (i.e., non-steroidal anti-inflammatory drugs). The chromatographic parameter can be helpful for the prediction of partition coefficients, i.e., AClogP, XlogP3, as well as logP of examined compounds.
本研究旨在通过反相薄层层析（RP-TLC）以及 Soczewiński-Wachtmeister 和 J. Ościk 方程评估选定的抗寄生虫药、抗高血压药和非甾体抗炎药（NSAIDs）的亲脂性。在各种色谱系统（即甲醇-水和丙酮-水）下获得的所有被检化合物的亲脂性参数，以及基于 Soczewiński-Wachtmeister 和 Ościk 方程（即 R 和 R）确定的参数，与理论参数（例如 AlogPs、AClogP、milogP、AlogP、MlogP、XlogP2、XlogP3）和分配系数（logP）的实验值进行了比较。结果发现，R 参数可作为描述高亲脂性和低亲脂性（即抗高血压药和抗寄生虫药）生物活性化合物亲脂性的替代工具。而 R 更适合中等亲脂性的化合物（即非甾体抗炎药）。色谱参数 有助于预测分配系数，如 AClogP、XlogP3 以及被检化合物的 logP。
