Abstract
Carbohydrates, traditionally known for their energy-providing role, have gained significant
attention in drug discovery due to their diverse bioactivities and stereodiversity.
However, pure carbohydrate molecules often exhibit limited bioactivity and suboptimal
chemical and physical characteristics. To address these challenges, functional groups
with bioactive scaffolds have been incorporated into carbohydrate to enhance their
bioactivity and improve their overall properties. Among the various synthetic methods
available, click chemistry has emerged as a powerful tool for the synthesis of carbohydrate-containing
bioactive scaffolds, known as glycohybrids. Click chemistry offers several advantages,
including high chemo- and regioselectivity, mild reaction conditions, easy purification,
and compatibility with multiple functional groups. In the present review, we have
emphasized the recent advances and most pertinent research on the development of 1,2,3-triazole-containing
glycohybrids using the click reaction, their biological evaluations and the structure-activity
relationship during 2017–2023. These newly synthesised glycohybrids could potentially
be developed as new chemical entities (NCE) in pharmaceutical chemistry and may encourage
the use of carbohydrates in drug discovery processes.
1 Introduction
2 CuAAC Click Chemistry Mediated Synthesis of Triazole-Based
Glycohybrids and their Biological Activities
3 Conclusions and Perspective
Keywords
regioselective - stereodivergent - glycohybrids - cycloaddition - triazole - glycoconjugates
- glucopyranoside - glycosidation
