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Mar. Drugs 2013, 11(9), 3297-3308; doi:10.3390/md11093297
Article

Natural and Semisynthetic Analogues of Manadoperoxide B Reveal New Structural Requirements for Trypanocidal Activity

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Received: 31 July 2013 / Revised: 16 August 2013 / Accepted: 19 August 2013 / Published: 28 August 2013
(This article belongs to the Special Issue Antiprotozoal Marine Natural Products)
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Abstract

Chemical analysis of the Indonesian sponge Plakortis cfr. lita afforded two new analogues of the potent trypanocidal agent manadoperoxide B (1), namely 12-isomanadoperoxide B (2) and manadoperoxidic acid B (3). These compounds were isolated along with a new short chain dicarboxylate monoester (4), bearing some interesting relationships with the polyketide endoperoxides found in this sponge. Some semi-synthetic analogues of manadoperoxide B (68) were prepared and evaluated for antitrypanosomal activity and cytotoxicity. These studies revealed crucial structure–activity relationships that should be taken into account in the design of optimized and simplified endoperoxyketal trypanocidal agents.
Keywords: manadoperoxide B; marine antitrypanosomals; structure–activity relationships manadoperoxide B; marine antitrypanosomals; structure–activity relationships
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Chianese, G.; Scala, F.; Calcinai, B.; Cerrano, C.; Dien, H.A.; Kaiser, M.; Tasdemir, D.; Taglialatela-Scafati, O. Natural and Semisynthetic Analogues of Manadoperoxide B Reveal New Structural Requirements for Trypanocidal Activity. Mar. Drugs 2013, 11, 3297-3308.

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