P200 Development of new antimalarial drugs : in vitro and in vivo antimalarial activity of endoperoxides
نویسندگان
چکیده
منابع مشابه
Cryptolepine and development of new antimalarial agents
Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...
متن کاملCryptolepine and development of new antimalarial agents
Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...
متن کاملPotent Antimalarial Activity of Acriflavine In Vitro and In Vivo
Malaria continues to be a major health problem globally. There is an urgent need to find new antimalarials. Acriflavine (ACF) is known as an antibacterial agent and more recently as an anticancer agent. Here, we report that ACF inhibits the growth of asexual stages of both chloroquine (CQ) sensitive and resistant strains of human malarial parasite, Plasmodium falciparum in vitro at nanomolar co...
متن کاملAminocyclopropanes as precursors of endoperoxides with antimalarial activity.
This contribution describes the synthesis of several novel bicyclic α-amino endoperoxides, including CF(3)-substituted compounds, prepared by the aerobic electrochemical oxidation of a family of bicyclic aminocyclopropanes. These, in turn, are readily synthesised by a titanium-mediated intramolecular cyclopropanation process (Kulinkovich-de Meijere reaction), starting from N-alkenyl amides that...
متن کاملThe mode of action of antimalarial endoperoxides.
The mechanism of action of artemisinin appears to involve two steps. In the first step, activation, intra-parasitic iron catalyses the cleavage of the endoperoxide bridge and the generation of free radicals. In the second step, alkylation, the artemisinin-derived free radical forms covalent bonds with parasite proteins.
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ژورنال
عنوان ژورنال: Medical Entomology and Zoology
سال: 2001
ISSN: 0424-7086,2185-5609
DOI: 10.7601/mez.52.127_4