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NMR-Based Fragment Screening in a Minimum Sample but Maximum Automation Mode

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Drug Discovery Based on Fluorine-Containing Glycomimetics.

Xingxing Wei¹, Pengyu Wang², Fen Liu²

¹Department of Pharmacy, Changzhi Medical College, No. 161, Jiefang East Street, Changzhi 046012, China.

Molecules (Basel, Switzerland)

|September 28, 2023

Summary

Fluorination enhances natural carbohydrates, creating stable and effective glycomimetics. This review details methods, effects, and biological activities of these modified sugars for improved therapeutic potential.

Keywords:

drug discovery fluorination glycomimetics physical properties synthesis

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Area of Science:

Carbohydrate Chemistry
Medicinal Chemistry
Glycobiology

Background:

Natural carbohydrates have limitations in stability and bioavailability.
Glycomimetics are synthetic analogs designed to overcome these limitations.
Fluorination offers a strategy to improve carbohydrate properties.

Purpose of the Study:

To review methods for preparing fluorinated carbohydrates.
To examine the impact of fluorination on carbohydrate characteristics.
To present the biological activities of fluorinated sugars.

Main Methods:

Literature review of fluorination techniques for carbohydrates.
Analysis of studies on the physical, chemical, and biological effects of fluorination.
Compilation of data on the biological activities of fluorinated carbohydrates.

Main Results:

Fluorination significantly enhances metabolic stability and bioavailability.
It can improve protein-binding affinity of carbohydrate analogs.
Various fluorination methods yield diverse fluorinated carbohydrate structures.

Conclusions:

Fluorinated carbohydrates represent a promising class of glycomimetics.
Fluorination is a valuable tool for optimizing carbohydrate-based therapeutics.
Further research into fluorinated sugars holds potential for new drug development.