Synthesis of Bioactive 1,2,3-Triazole-Fused Macrocycles via Azide-Alkyne Cycloaddition

Abstract A systematic highlight of syntheses reported since 2006 of 1,2,3-triazole-fused macrocycles possessing biological activities such as anticancer, antibacterial, antiviral, anti-inflammatory and antilarval action, is presented in this review. The well-renowned Cu-catalyzed azide-alkyne cycloaddition reaction was noted to be highly efficient and is one the most common methods utilized by scientists for the synthesis of 1,4-disubstituted triazole-fused macrocycles, whereas Ru-catalyzed cycloaddition is common for the formation of 1,5-disubstituted bioactive triazoles. This review would thus be extremely beneficial for both synthetic organic and medicinal chemists. 1 Introduction 2 Anticancer Derivatives 3 Antibacterial Derivatives 4 Derivatives with Dual Activity 5 Antilarval Derivatives 6 Anti-inflammatory Derivatives 7 Antiviral Derivatives 8 Anti-trypanosomal Derivatives 9 Derivatives with Miscellaneous Activities 10 Conclusion