Neoglycosylation and neoglycorandomization: Enabling tools for the discovery of novel glycosylated bioactive probes and early stage leads - PubMed (original) (raw)
Neoglycosylation and neoglycorandomization: Enabling tools for the discovery of novel glycosylated bioactive probes and early stage leads
Randal D Goff et al. Medchemcomm. 2014.
Abstract
This review focuses upon the development, scope, and utility of the highly versatile chemoselective alkoxyamine-based 'neoglycosylation' reaction first described by Peri and Dumy. The fundamentals of neoglycosylation and the subsequent development of a 'neoglycorandomization' platform to afford differentially-glycosylated libraries of plant-based natural products, microbial-based natural products, and small molecule-based drugs for drug discovery applications are discussed.
Conflict of interest statement
The authors report the following competing conflict of interest: J.S.T is a cofounder of Centrose (Madison, WI).
Figures
Figure 1
Neolgycosides by Peri and coworkers.,,,
Figure 2
Neoglycosides by Carrasco and André-Miral.–
Scheme 1
Comparison of conventional glycosylation strategy (A) to neoglycosylation (B)
Scheme 2
Chemoselective glycosylation between aminooxy-coupled compounds and aldehyde-containing sugars. (A) Anomeric-coupled glycopeptides reported by Mutter; (B) C6-coupled glycopeptides reported by Bertozzi.
Scheme 3
Mechanism of the neoglycosylation reaction involving reducing sugars and alkoxyamines (R1NHOR2).
Scheme 4
Typical methoxyamine handle installation on an aglycon.
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