Design and Synthesis of Iminosydnones for Fast Click and Release Reactions with Cycloalkynes
Emerging applications in the field of chemical biology are currently limited by the lack of bioorthogonal reactions allowing both removal and linkage of chemical entities on complex biomolecules. We recently discovered a novel reaction between iminosydnones and strained alkynes leading to two products resulting from ligation and fragmentation of iminosydnones under physiological conditions. We now report the synthesis of a panel of substituted iminosydnones and the structure reactivity relationship between these compounds and strained alkyne partners. This study identified the most relevant substituents, which allow to increase the rate of the transformation and to develop a bifunctional cleavable linker with improved kinetics.
Synthesis and biological activity evaluation of novel imidazolidinedione derivatives, as potent antidiabetic agent
A set of novel imidazolidinedione derivatives were synthesized and evaluated as potential antidiabetic agents. Imidazolidinedione scaffold-based molecules were synthesized and validated on a mice hyperglycemia model caused by alloxan. As a result, three of them showed antihyperglycemic activities. This research provides useful clues for further design and discovery of antidiabetic agents.