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

Molecules

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

Published: February 2022

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.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8838516PMC
http://dx.doi.org/10.3390/molecules27031003DOI Listing

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