期刊
MARINE DRUGS
卷 11, 期 9, 页码 3297-3308出版社
MDPI AG
DOI: 10.3390/md11093297
关键词
manadoperoxide B; marine antitrypanosomals; structure-activity relationships
资金
- EU project Bluegenics [311848]
- University of Naples Federico II (MOU)
- Universitas Sam Ratulangi, Manado
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.
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