aplysinopsin has been researched along with indole-3-carbaldehyde* in 1 studies
1 other study(ies) available for aplysinopsin and indole-3-carbaldehyde
Article | Year |
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Discovery of novel antileishmanial agents in an attempt to synthesize pentamidine-aplysinopsin hybrid molecule.
In an attempt to synthesize pentamidine-aplysinopsin hybrid molecule 25, a lead molecule 8 (containing Z-configured aplysinopsin moiety) was identified for antileishmanial activity. Optimization of lead 8 provided 24 (containing E-configured aplysinopsin) possessing 10 times more activity and 401-fold less toxicity than the drug pentamidine in cell based assays. Synthesis of 24 was possible, surprisingly, because of two innate reactivities of indole-3-carbaldehyde which provided it in diastereo- and regio-selectively pure form without recourse to the long reaction pathway. Topics: Animals; Antiprotozoal Agents; Cell Line; Drug Discovery; Indoles; Inhibitory Concentration 50; Leishmania donovani; Macrophages; Mice; Parasitic Sensitivity Tests; Pentamidine; Structure-Activity Relationship; Tryptophan | 2009 |