A Review of Modifications of Quinoline Antimalarials: Mefloquine and (hydroxy)Chloroquine

Kucharski, Dawid J.; Jaszczak, Michalina K.; Boratyński, Przemysław J.

doi:10.3390/molecules27031003

Open AccessReview

A Review of Modifications of Quinoline Antimalarials: Mefloquine and (hydroxy)Chloroquine

by

Dawid J. Kucharski

,

Michalina K. Jaszczak

and

Przemysław J. Boratyński

^*

Department of Organic and Medicinal Chemistry, Wrocław University of Technology, Wyspiańskiego 27, 50-370 Wrocław, Poland

^*

Author to whom correspondence should be addressed.

Molecules 2022, 27(3), 1003; https://doi.org/10.3390/molecules27031003

Submission received: 11 January 2022 / Revised: 27 January 2022 / Accepted: 31 January 2022 / Published: 2 February 2022

(This article belongs to the Special Issue Chemistry of Antiparasitic Drugs)

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Abstract

Late-stage modification of drug molecules is a fast method to introduce diversity into the already biologically active scaffold. A notable number of analogs of mefloquine, chloroquine, and hydroxychloroquine have been synthesized, starting from the readily available active pharmaceutical ingredient (API). In the current review, all the modifications sites and reactivity types are summarized and provide insight into the chemistry of these molecules. The approaches include the introduction of simple groups and functionalities. Coupling to other drugs, polymers, or carriers afforded hybrid compounds or conjugates with either easily hydrolyzable or more chemically inert bonds. The utility of some of the compounds was tested in antiprotozoal, antibacterial, and antiproliferative assays, as well as in enantiodifferentiation experiments.

Keywords: mefloquine; chloroquine; hydroxychloroquine; late-stage modification; semisynthesis; derivatization; quinoline

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MDPI and ACS Style

Kucharski, D.J.; Jaszczak, M.K.; Boratyński, P.J. A Review of Modifications of Quinoline Antimalarials: Mefloquine and (hydroxy)Chloroquine. Molecules 2022, 27, 1003. https://doi.org/10.3390/molecules27031003

AMA Style

Kucharski DJ, Jaszczak MK, Boratyński PJ. A Review of Modifications of Quinoline Antimalarials: Mefloquine and (hydroxy)Chloroquine. Molecules. 2022; 27(3):1003. https://doi.org/10.3390/molecules27031003

Chicago/Turabian Style

Kucharski, Dawid J., Michalina K. Jaszczak, and Przemysław J. Boratyński. 2022. "A Review of Modifications of Quinoline Antimalarials: Mefloquine and (hydroxy)Chloroquine" Molecules 27, no. 3: 1003. https://doi.org/10.3390/molecules27031003

APA Style

Kucharski, D. J., Jaszczak, M. K., & Boratyński, P. J. (2022). A Review of Modifications of Quinoline Antimalarials: Mefloquine and (hydroxy)Chloroquine. Molecules, 27(3), 1003. https://doi.org/10.3390/molecules27031003

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A Review of Modifications of Quinoline Antimalarials: Mefloquine and (hydroxy)Chloroquine

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