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Updated: Aug 5, 2026
05:07
Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Recent Advances in Pyrazole-Based Cholinesterase Inhibitors: Medicinal Chemistry Perspectives from 2020 to 2025
Lalsu Yeysin1, Deniz Akın2, Süleyman Çalışkan3
1Institute of Science, Gazi University, Ankara 06500, Türkiye.
Pharmaceuticals (Basel, Switzerland)
|July 28, 2026
Summary
Pyrazole derivatives show promise as cholinesterase inhibitors for Alzheimer's disease therapy. This review analyzes structure-activity relationships of these compounds, focusing on improving potency and drug-like properties.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Drug Discovery
Background:
- Pyrazole derivatives are versatile scaffolds for developing cholinesterase inhibitors.
- Their structural flexibility allows selective interaction with cholinesterase enzyme sites (CAS and PAS).
- These compounds are promising candidates for treating cognitive disorders, particularly Alzheimer's disease.
Purpose of the Study:
- To systematically review medicinal chemistry studies on pyrazole-based cholinesterase inhibitors (2020-2025).
- To analyze structure-activity relationships (SAR) of pyrazole core modifications.
- To evaluate trends in potency, selectivity, and drug-like characteristics.
Main Methods:
- Literature search across Scopus, PubMed, and Google Scholar.
- Analysis of in vitro enzymatic inhibition, molecular docking, and kinetic studies.
- Evaluation of ADME predictions and multi-target-directed ligand (MTDL) approaches.
Main Results:
- Detailed SAR analysis of structural alterations on the pyrazole core.
- Assessment of inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE).
- Identification of trends influencing compound potency, selectivity, and pharmacokinetic properties.
Conclusions:
- Pyrazole derivatives offer a viable strategy for developing novel Alzheimer's disease therapeutics.
- Addressing challenges in pharmacokinetics, blood-brain barrier penetration, and safety is crucial.
- Integrating rational design, computational modeling, and biological validation will accelerate clinical development.
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