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Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine.

ABSTRACT: Ionic liquids derived from classical antimalarials are emerging as a new approach towards the cost-effective rescuing of those drugs. Herein, we disclose novel surface-active ionic liquids derived from chloroquine and natural fatty acids whose antimalarial activity in vitro was found to be superior to that of the parent drug. The most potent ionic liquid was the laurate salt of chloroquine, which presented IC50 values of 4 and 110 nM against a chloroquine-sensitive and a chloroquine-resistant strain of Plasmodium falciparum, respectively, corresponding to an 11- and 6-fold increase in potency as compared to the reference chloroquine bisphosphate salt against the same strains. This unprecedented report opens new perspectives in both the fields of malaria chemotherapy and of surface-active ionic liquids derived from active pharmaceutical ingredients.

SUBMITTER: Silva AT

PROVIDER: S-EPMC7432003 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature

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Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine.

Silva Ana Teresa AT Lobo Lis L Oliveira Isabel S IS Gomes Joana J Teixeira Cátia C Nogueira Fátima F Marques Eduardo F EF Ferraz Ricardo R Gomes Paula P

International journal of molecular sciences 20200727 15

Ionic liquids derived from classical antimalarials are emerging as a new approach towards the cost-effective rescuing of those drugs. Herein, we disclose novel surface-active ionic liquids derived from chloroquine and natural fatty acids whose antimalarial activity in vitro was found to be superior to that of the parent drug. The most potent ionic liquid was the laurate salt of chloroquine, which presented IC<sub>50</sub> values of 4 and 110 nM against a chloroquine-sensitive and a chloroquine-r ...[more]

PMID: 32727096

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Project description:A new class of surface active ionic liquids (SAIL) have been reported to be a greener alternative to the conventional surfactants in enhanced oil recovery (EOR). These SAILs work efficiently under harsh salinity conditions encountered in the reservoir thereby recovering more additional oil during the tertiary oil recovery process. Adsorption mechanism of SAILs on different rock surface is however, not yet reported in the literature. This article highlights adsorption mechanism of three cationic SAILs having different headgroups, viz., imidazolium, pyridinium, pyrrolidinium, on different rock surfaces (crushed natural carbonate rock and crushed sandstone rock). All the SAILs studied here however had the same tail length and same anion (Br-) attached to it. XRD and XPS characterization techniques reveal that the crushed natural carbonate rock contains a substantial amount of silica, thus rendering it a slight negative charge. Static adsorption tests show that the retention efficiency on the natural carbonate type of rock for all the SAILs was lower than the conventional cationic surfactant, CTAB. The adsorption data obtained thereby was examined using four different adsorption isotherm models (Langmuir, Freundlich, Redlich-Peterson, and Sips). Results suggest that Sips adsorption isotherm model can satisfactorily estimate the adsorption of all the surface active agents on the natural carbonate rock. Factors like mineralogical composition of rock surface, presence of divalents, temperature, and structure of surfactants strongly affect the amount of surfactant adsorbed on reservoir rock. In order to evaluate the simultaneous effect all these factors as well as their interdependence on the retention capability of the three SAILs, a design of experiments approach has been employed further in this study. Statistical analysis of the data obtained after performing the full factorial experiments reveal that at high salinity, imidazoluim based SAIL show minimal adsorption on crushed natural carbonate rock at higher temperature. In general, at a given ionic strength, with increasing temperature as the amount of divalent in the aqueous solution increases, the amount of SAIL adsorbed on both the rock types decreases. Electrostatic attraction is the basic mechanism in governing adsorption of SAILs on the two types of rock surfaces. Results presented in this work can be used for EOR schemes.

Dataset Information

Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine.

Publications

Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine.

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