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13 - Electrical and Electronic Engineering, Metallurgy and Materials
University of Central Lancashire
The σ-Hole Phenomenon of Halogen Atoms Forms the Structural Basis of the Strong Inhibitory Potency of C5 Halogen Substituted Glucopyranosyl Nucleosides towards Glycogen Phosphorylase b
This is one of the relatively few papers to recognise the importance of halogen bonding/σ-hole effect in drug design efforts, and was highlighted for this reason in the article “Principles and applications of halogen bonding in medicinal chemistry and chemical biology” by Wilcken R et al., J Med Chem 2013, 56(4), 1363-1388. With respect to glycogen phosphorylase inhibition, the unravelling of deficiencies in the pharmacokinetic profile of the glucose derivatives studied will influence researchers in the design of more effective ‘drug-like’ analogues.