Motivated by the antimalarial properties observed in organic peroxides, an extensive series of glycosyl hydroperoxides was prepared with the aim of identifying new bioactive molecules. Selected compounds were tested against a Plasmodium falciparum culture (chloroquine-susceptible strain D10 and chloroquine-resistant strain W2). Screening results indicated that the factors critical for antimalarial activity were the presence of a hydroperoxide moiety and solubility in water at pH 5.0. Moreover, the ability to inhibit β-hematin formation in vitro has been evaluated (BHIA Assay).
Glycosyl hydroperoxides: a new class of potential antimalarial agents / B. Szechner, A. Jaromin, S. Parapini, N. Basilico, B. Grzeszczyk, B. Furman, M. Chmielewski. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 23:13(2015 Jul 01), pp. 3033-3039. [10.1016/j.bmc.2015.05.009]
Glycosyl hydroperoxides: a new class of potential antimalarial agents
S. Parapini;N. Basilico;
2015
Abstract
Motivated by the antimalarial properties observed in organic peroxides, an extensive series of glycosyl hydroperoxides was prepared with the aim of identifying new bioactive molecules. Selected compounds were tested against a Plasmodium falciparum culture (chloroquine-susceptible strain D10 and chloroquine-resistant strain W2). Screening results indicated that the factors critical for antimalarial activity were the presence of a hydroperoxide moiety and solubility in water at pH 5.0. Moreover, the ability to inhibit β-hematin formation in vitro has been evaluated (BHIA Assay).
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