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Target-based Antidiabetic Indole Derivatives and Insights into Structure-activity Relationships: A Mechanistic Update
Ankita Wal1, Pranay Wal1, Akanksha Gupta2
1PSIT-Pranveer Singh Institute of Technology (Pharmacy), Kanpur, India.
Current Drug Targets
|May 15, 2026
Summary
Indole derivatives show promise for treating type 2 diabetes mellitus by targeting multiple pathways. Further clinical studies are needed to optimize their use in personalized medicine.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Drug Discovery
Background:
- Type 2 diabetes mellitus (T2DM) is a growing global health concern.
- Existing T2DM therapies have limitations, necessitating novel interventions.
- Indole derivatives offer potential due to their adaptable structures and multi-target capabilities.
Purpose of the Study:
- To review recent advancements in indole-based antidiabetic agents.
- To analyze structure-activity relationships (SAR) and mechanistic insights.
- To evaluate the clinical viability and therapeutic potential of these compounds.
Main Methods:
- Systematic literature review (2020-2025) of PubMed, Scopus, and Web of Science.
- Inclusion of studies focusing on mechanistic insights, SAR, preclinical, and early clinical data.
- Analysis of identified indole derivatives targeting key diabetes pathways.
Main Results:
- Over 120 indole derivatives identified targeting pathways like AMPK activation, insulin sensitization, and enzyme inhibition (DPP-4, α-glucosidase).
- Specific structural modifications (N1, C2, C3, C5) significantly enhance bioactivity and selectivity.
- Innovations in synthesis, formulation (nanoparticles, prodrugs), and AI-driven design improve clinical potential.
Conclusions:
- Indole scaffolds exhibit polypharmacology, enabling multi-pathway modulation for hyperglycemia and complications.
- Challenges include toxicity, solubility, and translational gaps.
- Emerging delivery strategies and personalized medicine approaches hold promise for indole derivatives in T2DM treatment.
Keywords:
AIassisted drug designAMPK activationDPP-4 inhibitorsIndole derivativesantidiabetic agentsclinical trialsenzyme inhibitiongreen chemistry synthesis.insulin sensitizationnanoparticle formulationpersonalized medicinestructure activity relationship (SAR)targeted drug deliverytype 2 diabetes mellitus (T2DM)β-cell protection
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