Synthesis and anticonvulsant properties of new acetamide derivatives of phthalimide, and its saturated cyclohexane and norbornene analogs

Synthesis and anticonvulsant activity of new N-mannich bases derived from benzhydryl- and isopropyl-pyrrolidine-2,5-dione

“…Likewise, nine substances 5, 6, 7, 10, 11, 15, 17, 19, and 28 were effective only in the scPTZ test. Derivatives 5,7,9,11,12,13,15,17,19, and 28 showed protection at the dose of 100 mg/kg after 4 h. It is a better protection at thse same time point than the result of ethosuximide, recognized as the model antiepileptic drug effective in the scPTZ test. Especially interesting seem to be compounds 11 and 12, which revealed activity at the dose of 100 mg/kg not only after 4 h, but also after 0.5 h. The other compounds have demonstrated protection at the dose of 300 mg/kg after 4 h (6 and 10), and 0.5 h (compound 9).…”

“…Compounds 5,7,11,12,13,15, and 17, as well as ethosuximide and valproic acid compared with the vehicle-treated group, prolonged in a dose-dependent manner the latency time to first seizure episode. Compounds 5,7,11,12,13, and 17 at doses 100 and 150 mg/kg significantly prolonged latency time to the first seizure episode by 99-142% and 119-176%, respectively. Compound 15 at the dose of 150 mg/kg lengthened latency time to the first seizure episode by 128%, in a statistically significant manner, whereas reference compounds significantly prolonged latency time to the first seizure episode starting at the dose of 120 mg/kg (ethosuximide) or 250 mg/kg (valproic acid).…”

“…All compounds (5,7,9,11,12,13,15, and 17) showed higher potency in the scPTZ tests in comparison with the reference drugs -ethosuximide and valproic acid. Moreover, all these molecules demonstrated lower rotarod toxicity than phenytion, ethosuximide, and valproic acid, what resulted in more favorable protection indexes.…”

“…The results of elemental analyses were within ±0.4% of the theoretical values. 1 H NMR, 13 C NMR, and 19 F NMR spectra were obtained in a Varian Mercury spectrometer (Varian Inc., Palo Alto, CA), in CDCl 3 , operating at 300 MHz. Chemical shifts are reported in values (ppm) relative to TMS ¼ 0 ( 1 H), as an internal standard.…”

Synthesis, Characterization and Antimicrobial Evaluation of Newly Synthesized Compounds With Phthalimide Skeleton

“…Furthermore, many literatures have investigated the phthalimide derivatives due to their diverse range of biological activities such as antimicrobial [2][3][4][5], antiviral [6,7], anticancer [8,9], anti-inflammatory [10,11],antiepileptic [12,13], antihyperlipidimic [14,15], antihyperglycemic [16], anxiolytic [17], etc.…”