药物衍生的表面活性离子液体:一种显著提高伯氨喹血液期抗疟活性的经济有效方法。
Drug-Derived Surface-Active Ionic Liquids: A Cost-Effective Way To Expressively Increase the Blood-Stage Antimalarial Activity of Primaquine.
作者信息
Silva Ana Teresa, Oliveira Isabel S, Gomes Joana, Aguiar Luísa, Fontinha Diana, Duarte Denise, Nogueira Fátima, Prudêncio Miguel, Marques Eduardo F, Teixeira Cátia, Ferraz Ricardo, Gomes Paula
机构信息
LAQV-REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, Rua do Campo Alegre 687, 4169-007, Porto, Portugal.
CIQ-UP, Centro de Investigação em Química da Universidade do Porto, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, Rua do Campo Alegre 687, 4169-007, Porto, Portugal.
出版信息
ChemMedChem. 2022 Mar 4;17(5):e202100650. doi: 10.1002/cmdc.202100650. Epub 2021 Dec 23.
Inspired by previous disclosure of room-temperature ionic liquids derived from primaquine and cinnamic acids, which displayed slightly enhanced blood-stage activity compared to the parent drug, we have now combined this emblematic antimalarial with natural fatty acids. This affords surface-active ionic liquids whose liver-stage antiplasmodial activity is either retained or slightly enhanced, while revealing blood-stage antiplasmodial activity at least one order of magnitude higher than that of the parent compound. These findings open new perspectives towards the cost-effective recycling of classical drugs that are either shelved or in decline, and which is not limited to antimalarial agents.
受先前关于源自伯氨喹和肉桂酸的室温离子液体的披露启发,与母体药物相比,这些离子液体显示出略高的血液期活性,我们现在已将这种标志性抗疟药与天然脂肪酸结合。这产生了表面活性离子液体,其肝期抗疟活性得以保留或略有增强,同时显示出的血液期抗疟活性比母体化合物至少高一个数量级。这些发现为搁置或正在减少的经典药物的经济有效再利用开辟了新的前景,且这不仅限于抗疟药物。