Changing stroke rehab and research worldwide now.Time is Brain! trillions and trillions of neurons that DIE each day because there are NO effective hyperacute therapies besides tPA(only 12% effective). I have 523 posts on hyperacute therapy, enough for researchers to spend decades proving them out. These are my personal ideas and blog on stroke rehabilitation and stroke research. Do not attempt any of these without checking with your medical provider. Unless you join me in agitating, when you need these therapies they won't be there.

What this blog is for:

My blog is not to help survivors recover, it is to have the 10 million yearly stroke survivors light fires underneath their doctors, stroke hospitals and stroke researchers to get stroke solved. 100% recovery. The stroke medical world is completely failing at that goal, they don't even have it as a goal. Shortly after getting out of the hospital and getting NO information on the process or protocols of stroke rehabilitation and recovery I started searching on the internet and found that no other survivor received useful information. This is an attempt to cover all stroke rehabilitation information that should be readily available to survivors so they can talk with informed knowledge to their medical staff. It lays out what needs to be done to get stroke survivors closer to 100% recovery. It's quite disgusting that this information is not available from every stroke association and doctors group.

Friday, October 2, 2026

Design, synthesis, and biological evaluation of novel ebselen-chalcone hybrids as multifunctional neuroprotective agents for ischemic stroke

 

Maybe you want to get familiar with ebselen? Ask your doctor about it, no knowledge IS FUCKING INCOMPETENCE!

Ebselen, an anti-inflammatory antioxidant, was originally developed by Daiichi Sankyo, in Japan, to treat patients who had suffered a stroke. But the compound was never marketed and has since come off patent. It’s also part of the National Institutes of Health Clinical Collection—several hundred small molecules that have, to some extent, gone through the gamut of human clinical trials and have been found to be safe, but never reached final FDA approval.

  • ebselen (12 posts to December 2012)

Design, synthesis, and biological evaluation of novel ebselen-chalcone hybrids as multifunctional neuroprotective agents for ischemic stroke

Highlights

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    A total of 67 ebselen-chalcone hybrids were designed and synthesized based on a hybridization strategy.
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    C13 exhibited significant neuroprotective and anti-inflammatory activities with a marked safety.
  • •
    C13 showed exerted significant in vivo neuroprotective effect in a middle cerebral artery occlusion (MCAO) model.

Abstract

Ischemic stroke is a multifactorial neurological disorder characterized by oxidative stress, neuroinflammation, and mitochondrial dysfunction. Currently, effective neuroprotective agents for treating ischemic stroke remain limited. To integrate the glutathione peroxidase (GPx)-mimicking activity of ebselen with the antioxidant and anti-inflammatory properties of chalcones, a total of 67 ebselen-chalcone hybrids were rationally designed and synthesized. Biological evaluation identified B21 as an initial lead compound with improved neuroprotective activity and reduced cytotoxicity compared to ebselen, as reflected by an enhanced selectivity index (SI > 6.37 vs 2.43). Subsequent structural optimization led to the identification of C13, which exhibited superior neuroprotective and anti-inflammatory activities with a markedly improved safety (SI > 50.31). Furthermore, in vivo bioassay demonstrated that C13 showed good tolerability and exerted significant neuroprotective effects in a middle cerebral artery occlusion (MCAO) model, comparable to the positive control edaravone. Mechanistic studies revealed that C13 effectively reduced intracellular reactive oxygen species accumulation and preserved mitochondrial membrane potential, primarily through activation of the Nrf2/HO-1 signaling pathway. Overall, this study highlights the effectiveness of an ebselen-based molecular hybridization strategy and identifies C13 as a promising lead compound for ischemic stroke therapy.
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