Triazole Scaffolds as Privileged Bioisosteres in Drug Innovation: Synthetic Advances and Representative Applications (minireview)

Triazole frameworks, covering both 1,2,3-triazole and 1,2,4-triazole isomers, have been widely recognized as promising non-classical amide and carboxyl replacements in modern drug research. These nitrogen-rich heterocycles effectively resolve the metabolic instability and suboptimal physicochemical features commonly seen in conventional pharmacophores. This microreview collects representative advances achieved during 2021-2025, covering innovative synthetic routes and practical applications in drug structure optimization. Each example is narrated in around 200 words, emphasizing reaction design, mechanistic features, structural advantages, and therapeutic enhancements. The aim is to support the rational design, efficient preparation, and further exploration of triazole-containing drug candidates.

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Publication Details

Journal
Synlett
Published
2026-07-26
DOI
https://doi.org/10.1055/a-2923-9423
Primary Topic
Click Chemistry and Applications
Type
article
Field-Weighted Citation Impact
0.00

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article

Triazole Scaffolds as Privileged Bioisosteres in Drug Innovation: Synthetic Advances and Representative Applications (minireview)

Er‐Qing Li, Linlin Shi, Shuyue Bao
Synlett
Click Chemistry and Applications
article

Triazole Scaffolds as Privileged Bioisosteres in Drug Innovation: Synthetic Advances and Representative Applications (minireview)

Er‐Qing Li, Linlin Shi, Shuyue Bao
article en

Abstract

Triazole frameworks, covering both 1,2,3-triazole and 1,2,4-triazole isomers, have been widely recognized as promising non-classical amide and carboxyl replacements in modern drug research. These nitrogen-rich heterocycles effectively resolve the metabolic instability and suboptimal physicochemical features commonly seen in conventional pharmacophores. This microreview collects representative advances achieved during 2021-2025, covering innovative synthetic routes and practical applications in drug structure optimization. Each example is narrated in around 200 words, emphasizing reaction design, mechanistic features, structural advantages, and therapeutic enhancements. The aim is to support the rational design, efficient preparation, and further exploration of triazole-containing drug candidates.

Synlett
Zhengzhou University (CN)
National Natural Science Foundation of China, China Postdoctoral Science Foundation, Natural Science Foundation of Henan Province
Industry, innovation and infrastructure
Openalex Percentile: Top 16%
Click Chemistry and Applications
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