Question

Theoretical study on the molecular structure of Quinoline and its derivatives as an anti- malaria drug.

Answer 1

uinoline is used mainly as an intermediate in the manufacture of other products [1]. It is also used as a catalyst, a corrosion inhibitor, in metallurgical processes, in the manufacture of dyes, as a preservative for anatomical specimens, in polymers and agricultural chemicals, and as a solvent for resins and terpenes. It is also used as an antimalarial medicine. There is not much diversity in the application of quinoline but quinoline has various derivatives with a lot of applications, example is quinine. Quinine has antimalarial activities and is an alkaloid with plant origin. Some other derivatives of quinoline has antibiotic activities, example is 4-hydroxyl-2-alkylquinoline. Quinoline can therefore be said to have not only antimalarial properties but antibiotic activities as well. Quinoline-containing antimalarial drugs, such as chloroquine, quinine and mefloquine, are mainstays of chemotherapy against malaria. The molecular basis of the action of these drugs is not completely understood, but they are thought to interfere with the hemoglobin, in an acidic food vacuole, producing free heme and reactive oxygen species as toxic by-products. Polymerization neutralizes the heme moieties and detoxification of free radical species by a vulnerable series of antioxidant mechanisms. Chloroquine, a dibasic drug, is accumulated several thousand-fold in the food vacuole. The high intravacuolar chloroquine concentration is proposed to interfere with the polymerization of heme and/or the detoxification of the reactive oxygen species, effectively killing the parasite with its own metabolic waste. The more lipophilic quinoline methanol drugs, mefloquine and quinine do not appear to be concentrated so extensively in the food vacuole and may act on alternative targets in the parasite.
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