Marine endoperoxides as antimalarial lead compounds |
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Authors: | Ernesto Fattorusso Orazio Taglialatela-Scafati |
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Institution: | 1.Dipartimento di Chimica delle Sostanze Naturali,Università di Napoli “Federico II”,Naples,Italy |
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Abstract: | Malaria, a pathology caused by protozoa belonging to the genus Plasmodium, is one of the major threats to global health, with about 300–500 million new clinical cases occurring every year and 1–3
million annual deaths. The recrudescence in the number of fatal cases registered in recent years can be attributed to the
diffusion of multi-drug resistant strains of Plasmodium, which make less effective the limited armamentarium of available drugs. Living organisms are a recognized source of potentially
bioactive molecules and, among them, marine natural products are emerging as one of the most interesting sources to be exploited
for the discovery of new antimalarial compounds. In this article we will report results obtained for a single class of marine
metabolites, namely endoperoxide-containing derivatives. Many of these molecules possess a simple six-membered 1,2-dioxygenated
ring bearing two or three alkyl/aryl groups of different complexity. They can be divided according to the group linked at
one of the two endoperoxide-oxygen bearing carbons: peroxyketal derivatives (methoxy group) or non-peroxyketal derivatives
(methyl/ethyl groups). Molecules belonging to these classes show in vitro antimalarial activity in the nanomolar range on
chloroquine-resistant strains. A number of investigations gave insights into the mechanism of action of these molecules, suggesting
structural changes to optimize their antimalarial activity. |
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