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Structural modifications of N-1', N-3 '-disubstitued-2' H, 3H,5'H spiro-(2-benzofuran-1,4' -imidazolidine)-2',3,5' -triones and their anticonvulsant activities in the pilocarpine model of temporal lobe epilepsy

Posted on:2017-01-14Degree:Ph.DType:Dissertation
University:St. John's University (New York), School of PharmacyCandidate:Yang, ChenFull Text:PDF
GTID:1464390014475275Subject:Pharmaceutical sciences
Abstract/Summary:
Based on previous study of N-1', N-3'-disubstituted 2'H,3'H,5'H-spiro[2-benzofuran-1,4'imidazolidine]-2',3,5'-triones in anticonvulsant animal model, twenty-two new analogues were designed, synthesized and their anticonvulsant activities were evaluated in the pilocarpine model. Most of these compounds showed ability to protect against the high dose of pilocarpine-induced seizure. Compound 4g completely blocked the motor seizures. From SAR studies, a nitrophenyl group attached to N-1' and an n-propyl as well as a cyclopropyl group attached to N-3' were the most effective analogues.
Keywords/Search Tags:N-1', Anticonvulsant, Model
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