Publications by authors named "Amy Capes"
Article Synopsis
- The zinc-metalloenzyme GlcNAc-PI de-N-acetylase is crucial for producing mature GPI anchors in Trypanosoma brucei, the parasite behind African sleeping sickness.
- Researchers screened a library of compounds and found salicylic hydroxamic acid to be an effective inhibitor of this enzyme, marking it as the first small molecule inhibitor identified for the GPI pathway in trypanosomes.
- Analysis of how the structure influences the activity showed that the hydroxamic acid group and a hydroxyl group at the 2-position are vital for its effectiveness, while changes can be made at the 4- and 5-positions without losing potency.
Article Synopsis
- A series of 7 synthetic analogues were created to study their effects on GlcNAc-PI de-N-acetylase, an enzyme involved in producing glycosylphosphatidylinositol in Trypanosoma brucei, which is a target for drug development.
- The research focused on modifying components like D-myo-inositol and glucosamine, leading to the discovery that altering these structures affected their ability to serve as substrates or inhibitors for the enzyme.
- Key findings highlighted the critical role of phosphate in binding recognition and the influence of stereochemistry, informing future efforts to design effective enzyme inhibitors.
Article Synopsis
- The study expands the use of copper(II) tetrafluoroborate as a catalyst to open epoxides with various types of alcohols.
- It explores different solvents to enhance the reaction process during the catalytic opening.
- Additionally, the research includes a method for purifying the resulting products from these reactions.
Quinols have been developed as a class of potential anti-cancer compounds. They are thought to act as double Michael acceptors, forming two covalent bonds to their target protein(s). Quinols have also been shown to have activity against the parasite Trypanosoma brucei, the causative organism of human African trypanosomiasis, but they demonstrated little selectivity over mammalian MRC5 cells in a counter-screen.
View Article and Find Full Text PDFThe intramolecular iodo-aldol cyclization of alpha-substituted enoate aldehydes and ketones is described. Using prochiral starting materials, the reaction produces hetero- and carbocycles containing quaternary centers adjacent to secondary or tertiary centers. The reactions occur in good yields and are highly selective for the trans-products, having the hydroxyl and iodomethyl groups on opposite faces of the ring system.
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