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

Molecules

Przemysław J. Boratyński¹  Michalina K. Jaszczak¹  Dawid J. Kucharski¹ 

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

关键词: mefloquine;    chloroquine;    hydroxychloroquine;    late-stage modification;    semisynthesis;    derivatization;   

DOI  :  10.3390/molecules27031003

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown