Antibacterial Agent Synthesis

The rapid global incidence of infections caused by antibiotic-resistant bacterial pathogens is currently posing a serious threat to human health worldwide^[1]. This creates an urgent need to devote continuous efforts to the discovery and development of new antibacterial agents with a broad spectrum of activity and low toxicity. Click chemistry provides a powerful tool in the synthesis of antibacterial agents, as it allows efficient and clean creation of compounds under extremely mild conditions.

Applications

Over the past few years, click chemistry has been used in the synthesis of novel molecular targets that relate to inhibition of bacterial growth. Inulin is a group of abundant, water-soluble, renewable polysaccharides, which exhibit attractive biological activities and natural properties. Improvements such as chemical modification of inulin are often performed prior to further utilization. Dong et al^[2]. presented a method to modify inulin at its primary hydroxyls to synthesize amphiphilic aminated inulin by click chemistry to facilitate its chemical manipulation (Scheme 1). Additionally, antibacterial property of amphiphilic aminated inulin against Staphylococcus aureus (S. aureus) was evaluated and the best inhibitory index against S. aureus was 58% at 1 mg/ml. This study suggests that amphiphilic aminated inulin synthesized by click chemistry is a potential antibacterial agent. Similarly, Kant and co-workers synthesized novel triazole-based chalcone and flavone hybrid compounds by copper(I) catalyzed alkyne-azide cycloaddition (CuAAC) click reaction, and the antimicrobial activity of compounds was evaluated. The results showed that these triazole-based chalcone and flavone hybrid compounds exhibited better antimicrobial activity compared to the standard drugs[3].

Scheme 1. Synthetic pathway of amphiphilic aminated inulin.

What Can We Do?

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References

1. Kaur, J.; et al. An overview of recent advances in biomedical applications of click chemistry. Bioconjugate Chemistry. 2021, 8(32): 1455-1471.
2. Dong, F.; et al. Synthesis of amphiphilic aminated inulin via 'click chemistry' and evaluation for its antibacterial activity. Bioorganic & Medicinal Chemistry Letters. 2014, 24: 4590-4593.
3. Kant, R.; et al. Synthesis of newer 1,2,3-triazole linked chalcone and flavone hybrid compounds and evaluation of their antimicrobial and cytotoxic activities. European Journal of Medicinal Chemistry. 2016, 113: 34-49.