Smith, Garry R.; Brenneman, Douglas E.; Zhang, Yan; Du, Yanming; Reitz, Allen B. published the artcile< Small-Molecule Anticonvulsant Agents with Potent In Vitro Neuroprotection and Favorable Drug-Like Properties>, Synthetic Route of 2265-92-1, the main research area is difluoroethylsulfamide anticonvulsant neuroprotectant central nervous system pharmacokinetics pharmacodynamics.
Severe seizure activity is associated with reoccurring cycles of excitotoxicity and oxidative stress that result in progressive neuronal damage and death. Intervention with these pathol. processes is a compelling disease-modifying strategy for the treatment of seizure disorders. We have optimized a series of small mols. for neuroprotective and anticonvulsant activity as well as altered their phys. properties to address potential metabolic liabilities, to improve CNS penetration, and to prolong the duration of action in vivo. Utilizing phenotypic screening of hippocampal cultures with nutrient medium depleted of antioxidants as a disease model, cell death and decreased neuronal viability produced by acute treatment with glutamate or hydrogen peroxide were prevented. Modifications to our previously reported proof of concept compounds have resulted in a lead which has full neuroprotective action at <1 nM and antiseizure activity across six animal models including the kindled rat and displays excellent pharmacokinetics including high exposure to the brain. These modifications have also eliminated the requirement for a chiral mol., removing the possibility of racemization and making large-scale synthesis more easily accessible. These studies strengthen our earlier findings which indicate that potent, multifunctional neuroprotective anticonvulsants are feasible within a single mol. entity which also possesses favorable CNS-active drug properties in vitro and in vivo. Journal of Molecular Neuroscience published new progress about Anticonvulsants. 2265-92-1 belongs to class iodides-buliding-blocks, and the molecular formula is C6H3F2I, Synthetic Route of 2265-92-1.
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com