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Malaria is a disease caused by parasitic protozoa of the genus Plasmodium. Despite significant advances in understanding the disease and the parasite biology, malaria still remains one of the leading causes of morbidity and mortality, particularly in malaria-endemic regions of the world. The main factor hampering malaria control is the high degree of resistance developed by Plasmodium species against several classes of drugs. Artemisinin-based Combination Therapy (ACT) is the most rapidly acting antimalarial treatment effective against multi-drug resistant strains, and is, at present, the only group of antimalarial drugs to which resistance by Plasmodium falciparum has not developed yet in the field, even though the isolation of artemisinin-resistant strains is raising concern. As a result, discovering and developing novel antimalarial agents is one of the greatest challenges facing malaria control today. This review covers patent literature from 2007 to date regarding small molecules or natural compounds targeting the asexual forms of the parasite. Recent patents filed and issued for ameliorating conventional antimalarial treatment methods by non-conventional dosage forms are also reviewed.
Department of Pharmaceutical and Applied Chemistry, University of Siena, via Aldo Moro 2, 53100 Siena, Italy. @unisi.it.
This article was published in the following journal.
Name: Recent patents on anti-infective drug discovery
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A biguanide compound which has little antimalarial activity until metabolized in the body to the active antimalarial agent cycloguanil. The usefulness of proguanil is limited by the rapid development of drug resistance by the malarial parasite. The hydrochloride is used for the casual prophylaxis of falciparum malaria, to suppress other forms of malaria, and to reduce transmission of infection (From Martindale, The Extra Pharmacopoeia, 30th ed, p405)
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