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Design, Synthesis and Biological Evaluation of Indoline Derivatives as Multifunctional Agents for the Treatment of Ischemic Stroke
Open accessPreprint — published as 10.1007/s00044-022-02875-1 · Paper page
Abstract
In this work, a series of indoline derivatives as multifunctional neuroprotective agents for battling ischemic stroke were designed, synthesized, and biologically evaluated. In antioxidant assay, all compounds showed significant protective effects against H2O2-induced death of RAW 264.7 cells. In oxygen glucose deprivation/reperfusion (OGD/R)-induced neuronal damage, some compounds significantly elevated the cell survival rate. Among them, 7i, 7j and 7r exerted comparable neuroprotective effects to Ifenprodil, and exhibited binding affinity to N-methyl-D-aspartic acid receptors 2B (NMDA-GluN2B). At the concentrations of 0.1, 1 and 10 μM, 7i, 7j and 7r dose-dependently lowered the LPS-induced secretion of inflammatory cytokines, including TNF-α, IL-6 and NO, by BV-2 cells. Importantly, 7i and 7j can dramatically reduce the cerebral infarction rate and improve neurological deficit scores in middle cerebral artery occlusion (MCAO) rat model. As demonstrated by the above results, 7i and 7j are potential neuroprotective agents for the treatment of ischemic stroke.
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References 38 · Cited by 3
Metadata
- Authors
- Du, S., Jin, F., Li, J., Ma, X., Wang, H., & Qian, S.
- Affiliations
- Anhui University of Traditional Chinese Medicine (CN)
- Anhui University of Chinese Medicine
- Corresponding author
- Li, Jiaming
- Ma, Xiaodong
- Venue
- Medicinal Chemistry Research
- Published
- 2021-12-16
- Volume
- 31
- Issue
- 5
- Pages
- 805-818
- ISSN
- 1054-2523 (ISSN-L)
- OpenAlex
- W4225655087
- Cited by
- 3
- References
- 38
- Citations by year
- 2026: 2 · 2023: 1
- FWCI
- 0.09
- Type
- journal article
- Language
- en
- Open access
- green
- doi.org
- Locations
- Medicinal Chemistry Research (publishedVersion)
- Research Square (acceptedVersion, cc-by)
- Topics
- Life Sciences › Neuroscience › Neurology › Neuroprotection in Cerebral Ischemia
- Physical Sciences › Chemistry › Organic Chemistry › Heterocyclic Compound Synthesis and Bioactivity
- Life Sciences › Neuroscience › Neurology › Neuroinflammation and Neurodegeneration Mechanisms
- Keywords
- indoline derivatives, ischemic stroke, neuroprotection, antioxidant activity, oxygen-glucose deprivation/reoxygenation, neuroinflammation, inflammatory cytokines, middle cerebral artery occlusion, cerebral infarction, ifenprodil
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- Du, S., Jin, F., Li, J., Ma, X., Wang, H., & Qian, S. (2021). Design, Synthesis and Biological Evaluation of Indoline Derivatives as Multifunctional Agents for the Treatment of Ischemic Stroke. Medicinal Chemistry Research. https://doi.org/10.21203/rs.3.rs-1144423/v1
