4.5 Article

Study on the mechanism of action of artemether against schistosomes: The identification of cysteine adducts of both carbon-centred free radicals derived from artemether

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 13, Issue 10, Pages 1645-1647

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(03)00293-2

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Reaction of the antimalarial and anti-schistosome drug artemether (1) and catalytic amount of ferrous ion in the presence of excess cysteine gave two adducts of cysteine and previous postulated primary and secondary carbon-centred free radicals besides their other rearrangement products. This piece of further evidence for the presence of carbon-centred radicals, especially the secondary carbon-centred free radical for the first time by the isolation of its coupling adduct, will be help to understand the mechanism of action of artemether and other qinghaosu derivatives against parasites. (C) 2003 Elsevier Science Ltd. All rights reserved.

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