Design, Synthesis, and Antimicrobial Activities of 1,2,3-Triazole Glycoside Clickamers

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Microbiology

Background:

• Antimicrobial resistance is a critical global health challenge.
• There is an urgent need for novel antibacterial and antifungal agents.
• Carbohydrate-based compounds offer unique structural motifs for drug development.

Purpose of the Study:

• To synthesize novel aryl-substituted-1,2,3-triazoles linked to carbohydrates.
• To evaluate the in vitro antibacterial and antifungal activities of these synthesized compounds.
• To identify potent antimicrobial agents for combating resistant infections.

Main Methods:

• Synthesis of six novel aryl-substituted-1,2,3-triazoles via copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC).
• Characterization of synthesized compounds using spectroscopic techniques (e.g., NMR, Mass Spectrometry).
• In vitro antimicrobial assays against Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans, and Aspergillus niger, with Ampicillin and Nystatin as references.

Main Results:

• All synthesized triazole derivatives were confirmed by spectroscopic analysis.
• Staphylococcus aureus exhibited higher susceptibility to the tested compounds compared to other microbes.
• Several compounds demonstrated significant in vitro antifungal activity against Candida albicans and Aspergillus niger.

Conclusions:

• The synthesized carbohydrate-linked triazoles possess promising antibacterial and antifungal properties.
• The compounds are particularly effective against Staphylococcus aureus.
• This study highlights the potential of these novel triazoles as leads for developing new antimicrobial therapies.