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Heterocyclic compounds have been at the hierarchy position in academia, and
industrial arena, particularly the compounds containing triazole-core are found to be potent
with a broad range of biological activities. The resistance of triazole ring towards
chemical (acid and base) hydrolysis, oxidative and reductive reaction conditions, metabolic
degradation and its higher aromatic stabilization energy makes it a better heterocyclic
core as therapeutic agents. These triazole-linked compounds are used for clinical purposes
for antifungal, anti-mycobacterium, anticancer, anti-migraine and antidepressant
drugs. Triazole scaffolds are also found to act as a spacer for the sake of covalent attachment
of the high molecular weight bio-macromolecules with an experimental building
blocks to explore structure-function relationships. Herein, several methods and strategies
for the synthesis of compounds with 1,2,3-triazole moiety exploring Hüisgen, Meldal and Sharpless 1,3-dipolar
cycloaddition reaction between azide and alkyne derivatives have been deliberated for a series of representative
compounds. Moreover, this review article highlights in-depth applications of the [3+2]-cycloaddition reaction
for the advances of triazole-containing antibacterial as well as metabolic labelling agents for the in vitro and in
vivo studies on cellular level.
The copper‐catalyzed oxidative azide‐olefin cycloaddition (OAOC) reaction of differently substituted α,β‐unsaturated carbonyls with azides provided an efficient method for preparing biologically active 1,4,5‐trisubstituted 1,2,3‐triazoles. In this study, the cycloaddition reaction was found to be a simple and powerful method for constructing diverse mono‐ and bis‐(1,4,5‐trisubstituted 1,2,3‐triazole) functionalized heterocyclic compounds in moderate to high yields with great regioselectivity. The XRD‐analysis data of one of the bis‐triazole derivatives supported the regioselectivity as well as the conformity of the method in the construction of the triazole nucleus. The preliminary antifungal profile against C. albicans was observed with cinnamaldehyde‐based triazole derivatives demonstrating promising results.
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