Abram, Michal; Rapacz, Anna; Mogilski, Szczepan; Latacz, Gniewomir; Lubelska, Annamaria; Kaminski, Rafal M.; Kaminski, Krzysztof published the artcile< Multitargeted Compounds Derived from (2,5-Dioxopyrrolidin-1-yl)(phenyl)-Acetamides as Candidates for Effective Anticonvulsant and Antinociceptive Agents>, Recommanded Product: (3-Bromophenyl)(trifluoromethyl)sulfane, the main research area is epilepsy neuropathic pain anticonvulsant antinociceptive multitargeted drugs hybrid compound; Hybrid compounds; anticonvulsant activity; antinociceptive activity; epilepsy; multitargeted drugs; neuropathic pain.
We developed a focused set of original hybrid pyrrolidine-2,5-dione derivatives with potent anticonvulsant and antinociceptive properties. These hybrid compounds demonstrated broad-spectrum protective activity in a range of mouse models, such as the maximal electroshock (MES) test, the pentylenetetrazole-induced seizures (scPTZ), and the 6 Hz (32 mA) seizures. Compound 22(I) showed the most potent anticonvulsant activity (ED50 MES = 23.7 mg/kg, ED50 6 Hz (32 mA) = 22.4 mg/kg, ED50scPTZ = 59.4 mg/kg). In addition, 22 revealed potent efficacy in the formalin-induced tonic pain. These in vivo activities of 22 are likely mediated by several targets and may result from the inhibition of central sodium/calcium currents and transient receptor potential vanilloid 1 (TRPV1) receptor antagonism. Finally, the lead compound 22 revealed drug-like absorption, distribution, metabolism, excretion, toxicity (ADME-Tox) properties in the in vitro assays, making it a potential candidate for further development in epilepsy and neuropathic pain indications.
ACS Chemical Neuroscience published new progress about Analgesics. 2252-45-1 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3S, Recommanded Product: (3-Bromophenyl)(trifluoromethyl)sulfane.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary