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Fused 1H-/2H-Indazole as Bioactive Privileged Scaffolds: Synthetic Strategies and Pharmaceutical Applications
Richa Sharma1,2, Amol T Mahajan3, Vidit Shrivastava3
1Laboratory of Organic and Medicinal Chemistry (OMC Lab), Department of Chemistry, Malaviya National Institute of Technology, Jawaharlal Nehru Marg, Jaipur, 302017, India.
Current Drug Discovery Technologies
|May 21, 2026
Summary
Indazole derivatives are crucial in drug discovery, offering diverse pharmacological activities. Innovative C-H functionalization strategies are accelerating the development of novel indazole-based pharmaceuticals.
Area of Science:
- Medicinal Chemistry
- Organic Chemistry
- Drug Discovery
Background:
- Bioheterocycles, particularly indazoles, are vital in pharmaceuticals due to their wide-ranging medicinal applications.
- The indazole scaffold is present in natural products and numerous clinically used drugs, highlighting its significance.
- Indazoles exhibit diverse pharmacological activities, including anticancer, anti-inflammatory, and neuroprotective effects.
Purpose of the Study:
- To explore innovative C-H functionalization strategies for synthesizing bioactive indazole derivatives.
- To provide a comprehensive understanding of indazole's role in drug design and development.
Main Methods:
- Review of conventional and modern synthetic routes for indazole derivatives.
- Focus on C-H functionalization techniques for efficient molecular elaboration.
- Analysis of structure-activity relationships of indazole-based compounds.
Main Results:
- C-H functionalization significantly accelerates the design and development of novel indazole derivatives.
- Identified key synthetic pathways for accessing diverse indazole scaffolds.
- Highlighted the broad therapeutic potential of newly developed indazole compounds.
Conclusions:
- Innovative C-H functionalization strategies are pivotal in advancing indazole-based drug discovery.
- The indazole framework remains a highly promising scaffold for developing new pharmaceuticals.
- Further research into C-H functionalization will unlock new therapeutic agents.

