# Synthesis of novel pyrazole derivatives and neuroprotective effect investigation

**Authors:** Aihua Feng, Qing Zeng, Jun Wang, Han Li, Xu Fang, Yan Geng, Wei Pan, Gang Li, Junfeng Dong

PMC · DOI: 10.1080/14756366.2025.2583820 · Journal of Enzyme Inhibition and Medicinal Chemistry · 2025-11-12

## TL;DR

This paper reports the synthesis of new pyrazole compounds that show strong anti-inflammatory effects, potentially useful for treating spinal cord injuries.

## Contribution

The study introduces novel pyrazole derivatives with potent anti-inflammatory activity, particularly compound 6g, which outperforms existing drugs.

## Key findings

- Compound 6g showed the strongest anti-inflammatory effect among the synthesized pyrazole derivatives.
- Compound 6g exhibited better IL-6 suppression than dexamethasone and Celecoxib without significant cytotoxicity.

## Abstract

Spinal cord injuries (SCIs) cause irreversible damage and lasting neurological impairments. Current treatments are limited to surgical and pharmaceutical interventions, underscoring the need for novel agents. In this study, 27 novel pyrazole derivatives were designed, synthesised. The anti-inflammatory and antioxidant activities of the compounds were systematically evaluated utilising lipopolysaccharide-stimulated BV2 microglial cells. Anti-inflammatory activity was assessed by quantifying the mRNA expression levels of key pro-inflammatory cytokines [tumour necrosis factor-α, interleukin-1β, and interleukin-6 (IL-6)] via quantitative reverse transcription polymerase chain reaction. Among the synthesised derivatives, compound 6g demonstrated the most potent anti-inflammatory effect, exhibiting an IC50 value of 9.562 μM for the suppression of IL-6 expression and no significant cytotoxicity was observed. Notable, compound 6g exhibited better inhibitory potency against IL-6 expression compared to the anti-inflammatory drugs dexamethasone and Celecoxib. These findings strongly support the potential of compound 6g as a promising therapeutic candidate for mitigating secondary inflammation in SCI.

## Linked entities

- **Chemicals:** dexamethasone (PubChem CID 5743), Celecoxib (PubChem CID 2662)

## Full-text entities

- **Genes:** Il1b (interleukin 1 beta) [NCBI Gene 16176] {aka IL-1beta, Il-1b}, Il6 (interleukin 6) [NCBI Gene 16193] {aka Il-6}
- **Diseases:** inflammation (MESH:D007249), neurological impairments (MESH:D009422), cytotoxicity (MESH:D064420), SCIs (MESH:D013119)
- **Chemicals:** lipopolysaccharide (MESH:D008070), pyrazole (MESH:C031280), Celecoxib (MESH:D000068579), dexamethasone (MESH:D003907)
- **Cell lines:** BV2 — Mus musculus (Mouse), Transformed cell line (CVCL_0182)

## Full text

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## Figures

11 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12613307/full.md

## References

44 references — full list in the complete paper: https://tomesphere.com/paper/PMC12613307/full.md

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Source: https://tomesphere.com/paper/PMC12613307