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

Chianese, Giuseppina, Scala, Fernando, Calcinai, Barbara, Cerrano, Carlo, Dien, Henny A., Kaiser, Marcel, Tasdemir, Deniz and Taglialatela-Scafati, Orazio (2013) Natural and Semisynthetic Analogues of Manadoperoxide B Reveal New Structural Requirements for Trypanocidal Activity. Open Access Marine Drugs, 11 (9). pp. 3297-3308. DOI 10.3390/md11093297.

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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 (6-8) 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.

Document Type: Article
Keywords: manadoperoxide B; marine antitrypanosomals; structure–activity relationships
Refereed: Yes
Open Access Journal?: Yes
Publisher: MDPI
Date Deposited: 27 Aug 2014 09:18
Last Modified: 14 Jul 2020 11:46
URI: https://oceanrep.geomar.de/id/eprint/23454

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