A Study of Fasoracetam’s Solid State Forms: A Potential Anti-Alzheimer Pharmaceutical

Harmsen, Bram; Robeyns, Koen; Leyssens, Tom

doi:10.1016/j.xphs.2017.01.016

Cited by 4 publications

(1 citation statement)

References 26 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Calculated water space for fasoracetam monohydrate (CSD refcode PAPNIG; Harmsen et al, 2017) with water molecules occupying discrete pockets within the crystal structure.…”

Section: Figurementioning

confidence: 99%

Mercury 4.0: from visualization to analysis, design and prediction

et al. 2020

View full text Add to dashboard Cite

The program Mercury, developed at the Cambridge Crystallographic Data Centre, was originally designed primarily as a crystal structure visualization tool. Over the years the fields and scientific communities of chemical crystallography and crystal engineering have developed to require more advanced structural analysis software. Mercury has evolved alongside these scientific communities and is now a powerful analysis, design and prediction platform which goes a lot further than simple structure visualization.

show abstract

“…Calculated water space for fasoracetam monohydrate (CSD refcode PAPNIG; Harmsen et al, 2017) with water molecules occupying discrete pockets within the crystal structure.…”

Section: Figurementioning

confidence: 99%

Mercury 4.0: from visualization to analysis, design and prediction

et al. 2020

View full text Add to dashboard Cite

show abstract

Thermal characterization and stability evaluation of leishmanicidal selenocyanate and diselenide derivatives

Etxebeste

Durán

Sanmartín

et al. 2021

J Therm Anal Calorim

View full text Add to dashboard Cite

A Novel Phenylpyrrolidine Derivative: Synthesis and Effect on Cognitive Functions in Rats with Experimental Ishemic Stroke

et al. 2021

View full text Add to dashboard Cite

We performed an in silico, in vitro, and in vivo assessment of a potassium 2-[2-(2-oxo-4-phenylpyrrolidin-1-yl) acetamido]ethanesulfonate (compound 1) as a potential prodrug for cognitive function improvement in ischemic brain injury. Using in silico methods, we predicted the pharmacological efficacy and possible safety in rat models. In addition, in silico data showed neuroprotective features of compound 1, which were further supported by in vitro experiments in a glutamate excitotoxicity-induced model in newborn rat cortical neuron cultures. Next, we checked whether compound 1 is capable of crossing the blood–brain barrier in intact and ischemic animals. Compound 1 improved animal behavior both in intact and ischemic rats and, even though the concentration in intact brains was low, we still observed a significant anxiety reduction and activity escalation. We used molecular docking and molecular dynamics to support our hypothesis that compound 1 could affect the AMPA receptor function. In a rat model of acute focal cerebral ischemia, we studied the effects of compound 1 on the behavior and neurological deficit. An in vivo experiment demonstrated that compound 1 significantly reduced the neurological deficit and improved neurological symptom regression, exploratory behavior, and anxiety. Thus, here, for the first time, we show that compound 1 can be considered as an agent for restoring cognitive functions.

show abstract

A Study of Fasoracetam’s Solid State Forms: A Potential Anti-Alzheimer Pharmaceutical

Cited by 4 publications

References 26 publications

Mercury 4.0: from visualization to analysis, design and prediction

Mercury 4.0: from visualization to analysis, design and prediction

Thermal characterization and stability evaluation of leishmanicidal selenocyanate and diselenide derivatives

A Novel Phenylpyrrolidine Derivative: Synthesis and Effect on Cognitive Functions in Rats with Experimental Ishemic Stroke

Contact Info

Product

Resources

About