Chemoselective Formation and Reaction of Densely Functionalised Bicyclic Tetramic Acids and Their Biological Activity
| Autor: | Amber L. Thompson, Laia Josa-Culleré, Mark G. Moloney, Christopher Towers |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
Bicyclic molecule
biology 010405 organic chemistry Chemistry Stereochemistry Gram-positive bacteria Organic Chemistry chemistry.chemical_element Biological activity Calcium 010402 general chemistry biology.organism_classification 01 natural sciences 0104 chemical sciences chemistry.chemical_compound Amide Proteasome inhibitor medicine Physical and Theoretical Chemistry Chemoselectivity medicine.drug |
| Zdroj: | European Journal of Organic Chemistry. 2017:7055-7059 |
| ISSN: | 1434-193X |
| Popis: | Weinreb amide derivatives of tetramates may be effectively accessed by chemoselective Dieckmann reaction, and further react with Grignards in a fully chemoselective reaction, giving rise to unsaturated acyl derivatives not easily available by other routes. These systems are strong chelators of calcium, and some show potent activity against Gram positive bacteria, and one is a first-in-class proteasome inhibitor. |
| Databáze: | OpenAIRE |
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