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- W2952378930 abstract "Malaria remains one of the most widespread health threats in the tropics. It is estimated that there are 300 to 500 million cases of malaria every year and around two million deaths [1]. The major concern in the treatment of this plague is the spread of resistance of Plasmodium falciparum to the very limited arsenal of antimalarial drugs. This situation appeals for the development of novel antimalarial leads [2]. Therefore, we investigated the in vitro antimalarial activities of drugs from our library containing N1,N4-quinoxaline dioxide derivatives, which were previously shown to have good antituberculosis activity [3–5]. Structures related to this heterocycle system have important biological activity and their biodisponibility and toxicity depend on the presence of substitutes in the lateral chains [6]. In order to better understand the mechanism of action of the compounds evaluated herein, we also determinated their ability to interfere with the ferriprotoporphyrin (FP) biomineralization process, a fundamental metabolism process of Plasmodium [7]. The results of activity assays, along with the comparative potency index relative to the reference drug (chloroquine), are summarized in the Table. The relation between structure and activity are related to the presence of Cl on position 7 (frequently found in active compounds as chloroquine), an amine situated in lateral chain and the 1,4-di-N-oxide system. The importance of cyano moiety in position 2 will be studied later. From data in the Table, it can easily be deduced that the presence of a piperazine ring is essential for the antimalarial activity. In 4a, the 2-methoxy group promoted the highest activity (IC50 1.25 higher than chloroquine). When a chloride replaced this group in position 4, for compound 4b, the antimalarial activity decreased dramatically (IC50 20 times higher than chloroquine). A weak antimalarial product, 5, (IC50 30 times higher than chloroquine) was obtained" @default.
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- W2952378930 date "2003-01-01" @default.
- W2952378930 modified "2023-09-29" @default.
- W2952378930 title "Anti-malarial activity of some 7-chloro-2-quinoxalinecarbonitrile-1,4-di-N-oxide derivatives." @default.
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