Design, synthesis and biological evaluation of indoline derivatives as multifunctional agents for the treatment of ischemic stroke

نویسندگان

چکیده

In this work, a series of indoline derivatives as multifunctional neuroprotective agents for battling ischemic stroke were designed, synthesized, and biologically evaluated. antioxidant assay, all compounds showed significant protective effects against H2O2-induced death RAW 264.7 cells. oxygen glucose deprivation/reperfusion (OGD/R)-induced neuronal damage, some significantly elevated the cell survival rate. Among them, 7i, 7j 7r exerted comparable to ifenprodil, exhibited binding affinity N-methyl-D-aspartic acid receptors 2B (NMDA-GluN2B). At concentrations 0.1, 1 10 μM, dose-dependently lowered LPS-induced secretion inflammatory cytokines, including TNF-α, IL-6 NO, by BV-2 Importantly, 7i can dramatically reduce cerebral infarction rate improve neurological deficit scores in middle artery occlusion (MCAO) rat model. As demonstrated above results, are potential treatment stroke.

برای دانلود رایگان متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis and biological evaluation of novel indoline-2,3-dione derivatives as antitumor agents.

A new series of 1,5-disubstituted indolin-2,3-diones was synthesized and their inhibition of the growth of a human acute promyelocytic leukemia (HL-60) cell line was evaluated. These compounds had promising inhibition of HL-60 cell growth in vitro. Results indicated that compounds with a benzyl substituent at the N-1 position on the indolin-2,3-dione ring had more potent antiproliferative activ...

متن کامل

Synthesis and evaluation of paeonol derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.

Alzheimer's disease (AD) is a progressive neurodegenerative brain disorder characterized by memory loss, language impairment, personality changes and intellectual decline. Taking into account the key pathological features of AD, such as low levels of acetylcholine, beta-amyloid (Aβ) aggregation, oxidative stress and dyshomeostasis of biometals, a new series of paeonol derivatives 5a-5d merging ...

متن کامل

Synthesis and Biological Evaluation of Novel Quinoline Derivatives as Antibacterial and Antifungal Agents

Vilsmeier Several diamide derivatives containing 2-chloroquinoline scaffolds were synthesized via Ugi reaction of 2-chloroquinoline-3-carboxaldehydes, amines, carboxylic acids and isocyanides. The diversity of these quinolinyl Ugi-adducts was increased by using 2-chloroquinoline-3-carboxylic acids as a source of acid. Among them, compounds 2d, 2n, 2p, 4a, 4c and<strong...

متن کامل

Design, Synthesis, Biological Evaluation and Molecular Modeling Study of Novel Indolizine-1-Carbonitrile Derivatives as Potential Anti-Microbial Agents

A novel one-pot two step tandem reaction for the synthesis of indolizine-1-carbonitrile derivatives (5a-i) was identified. The route comprises 1,3-dipolar cycloaddition reaction of aromatic aldehyde derivatives (1a-i), malononitrile (2) and 1-(2-(4-bromophenyl)-2-oxoethyl)-2-chloropyridin-1-ium (4) under ultrasound irradiation at room temperature in the presence of triethylamine at acetonitrile...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

ژورنال

عنوان ژورنال: Medicinal Chemistry Research

سال: 2022

ISSN: ['1554-8120', '1054-2523']

DOI: https://doi.org/10.1007/s00044-022-02875-1