Natural and semisynthetic analogues of manadoperoxide B reveal new structural requirements for trypanocidal activity

Mar Drugs. 2013 Aug 28;11(9):3297-308. doi: 10.3390/md11093297.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Plakortis / chemistry*
  • Porifera / chemistry*
  • Structure-Activity Relationship
  • Trypanocidal Agents / chemistry*
  • Trypanocidal Agents / pharmacology*

Substances

  • Trypanocidal Agents