Drugs effective against the erythrocyte stage of plasmodia infection

4-Aminoquinolines and quinolinmethanols

In the erythrocyte stage of plasmodia infection, two classes of drugs are used: 4-amino-quinolines and quinolinmethanols. 4-Aminoquinolines (chloroquine, amodiaquin, and hydroxychloroquine) are synthetic compounds. Their most important structural characteristic is the type of substituent at C7 and C4 of the quinoline ring. It has been shown that an amine substituent is necessary at C4 of the quinoline ring, which can vary while retaining antimalarial activity of the compound; however, the necessary conditions for expression of antimalarial activity is the presence of a chlorine atom at C7 of the quinoline ring. The prototype of this group of compounds is chloroquine. The second group of drugs used during the erythrocyte stage of malarial infections is quinolinmethanol derivatives. This group includes mefloquine, pyranobenzodioxepin derivative isolated from the plant—quinghaosu, as well as cinchona alkaloids that are made from the bark of the cinchona tree, of which only quinine is still used for treating malaria.

Chloroquine: Chloroquine, 7-chloro-4-(4-diethylamino-1-methylbutylamino)-quinoline (37.1.3), is made by reacting 4,7-dichloroquinoline (37.1.1.1) with 4-diethylamino-1-methylbutylamine (37.1.1.2) at 180 °C [1-3].

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