2. Academic Validation
  3. Identification of 3-methyl-1-(3-methylpyridin-2-yl)-1H-pyrazol-5-ol as promising neuroprotective agent

Identification of 3-methyl-1-(3-methylpyridin-2-yl)-1H-pyrazol-5-ol as promising neuroprotective agent

  • Bioorg Med Chem Lett. 2024 Oct 10:114:129983. doi: 10.1016/j.bmcl.2024.129983.
Peng Zhu 1,  Yulu Wu 1,  Zhikang Du 2,  Siyi Li 1,  Jiaming Li 1,  Xin Lu 3,  Xueyang Jiang 4
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, Anhui University of Chinese Medicine, Hefei 230012, China.
  • 2 Institute of Translational Medicine, School of Medicine, Yangzhou University, Yangzhou 225009, China.
  • 3 Institute of Translational Medicine, School of Medicine, Yangzhou University, Yangzhou 225009, China; Jiangsu Key Laboratory of Integrated Traditional Chinese and Western Medicine for Prevention and Treatment of Senile Diseases, Yangzhou University, Yangzhou 225009, China.
  • 4 Department of Medicinal Chemistry, Anhui University of Chinese Medicine, Hefei 230012, China. Electronic address: jiang0568@126.com.
PMID: 39395634 DOI: 10.1016/j.bmcl.2024.129983
Abstract

Pyrazolol derivatives are gaining significant attention for their diverse pharmacological effects, such as analgesic, anti-inflammatory, antioxidant, and Anticancer activities. In this study, 20 pyrazolol derivatives were designed and synthesized to develop an anti-ischemic stroke formulation with free radical scavenging activity. Most of these synthesized compounds demonstrated antioxidant capabilities in DPPH, ABTS radical scavenging, and ORACFL assays. The methyl-substituted compound Y12, in particular, showed exceptional antioxidant capacity. Additionally, these compounds showed excellent neurocytoprotective effects in the SH-SY5Y cell injury model subjected to oxygen-glucose deprivation/reoxygenation (OGD/R). Notably, Y12 exhibited significant metal chelating activity with Cu2+. In vivo studies confirmed that compound Y12 has neuroprotective effects and can significantly reduce the infarct area in a mouse model of focal cerebral ischemia induced by transient middle cerebral artery occlusion (tMCAO).

Keywords

Cerebral ischemia; Free radical scavenging; Neuroprotection; Pyrazolol.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z