Nine C-1 and C-2 fluorinated castanospermines were synthesized efficiently, and the C-2 fluorinated derivatives were found to be potent and specific α-glucosidase inhibitors, owing to fluorine-induced reestablishment of docking modes in the enzyme.
We summarized the development of macrocycle-carbohydrate conjugates and their biomedical application in the past decade, and provided our contention regarding the future trend of this topic.
Parallel FluoPol-ABPP screenings on lysosomal β-glucosidase (GBA1) and α-glucosidase (GAA) revealed a N-9-phenanthrenyl-DNJ that inhibits GAA selectively and is an interesting hit for the development of chaperones for Pompe disease.
The Ugi–Joullié three-component reaction evolved from the classic Ugi four-component reaction and enables the facile and efficient formation of polysubstituted nitrogen heterocycles from cyclic imines, isonitriles and carboxylic acids.
In this article, we provide a comprehensive review of the main sources and biosynthesis pathways of 1-dnj, strategies to increase its production, and the therapeutic effects and mechanisms of 1-dnj on diabetes mellitus (DM) and various diabetic complications.