Department of Pharmaceutical and Therapeutic Chemistry, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science and Technology of Târgu Mureș, 540142 Târgu Mureș, Romania.
Molecules. 2022 Jun 3;27(11):3601. doi: 10.3390/molecules27113601.
Chirality is becoming an essential issue in modern pharmaceutical research as regulatory agencies emphasize the safety and efficiency of enantiomers in drug development. The development of efficient and reliable chiral separation methods became a necessity in the last 30 years, and capillary electrophoresis (CE), due to its relatively low costs and "green" features, is attracting increased attention. Cyclodextrin (CD) and their derivatives are the most frequently used chiral selectors (CSs) in CE, however, the use of antibiotics as CSs represents an interesting alternative. Various classes of antibiotics (aminoglycosides, ansamycins, glycopeptides, lincosamides, macrolides, tetracyclines) have been used more or less successfully for the enantio-separation of pharmaceuticals. Antibiotics offer the possibility of a multitude of potential interactions (electrostatic, inclusion, hydrogen bonding, etc.) due to their chemical diversity, allowing the enantio-separation of analytes with a wide range of structural characteristics. This article aims to review the application of various classes of antibiotics in the CE enantio-separation of pharmaceuticals. Antibiotic physiochemical characteristics, variables impacting enantio-separation, advantages, and disadvantages when certain antibiotics are used as CSs in CE are also explored.
手性在现代药物研究中变得越来越重要,因为监管机构强调了在药物开发中对映异构体的安全性和效率。在过去的 30 年中,开发高效、可靠的手性分离方法成为一种必要,由于毛细管电泳(CE)具有相对较低的成本和“绿色”特点,因此越来越受到关注。环糊精(CD)及其衍生物是 CE 中最常用的手性选择剂(CSs),但是,将抗生素用作 CSs 代表了一种有趣的替代方法。各种类型的抗生素(氨基糖苷类、安莎霉素类、糖肽类、林可酰胺类、大环内酯类、四环素类)或多或少已成功地用于药物的对映体分离。由于抗生素的化学多样性,它们提供了多种潜在相互作用的可能性(静电、包含、氢键等),从而允许对具有广泛结构特征的分析物进行对映体分离。本文旨在综述各种类型的抗生素在 CE 药物对映体分离中的应用。还探讨了抗生素的理化特性、影响对映体分离的变量、在 CE 中将某些抗生素用作 CSs 的优点和缺点。