This study investigated the anticonvulsant activity of a new phthalazine tetrazole derivative, QUAN-0808 (6-(4-chlorophenoxy)-tetrazolo[5,1-a]phthalazine), in the mouse maximal electroshock (MES) seizure model. The neurotoxicity of QUAN-0808 was investigated using the rotarod neurotoxicity test in mice. QUAN-0808 exhibited higher activity (median effective dose, ED(50) = 6.8 mg/kg) and lower ne...

Several heteroaryl semicarbazones were prepared by the reaction of heteroaryl hydrazine carboxamide with aryl aldehydes or ketones. The structures of the synthesized compounds were confirmed by spectral data and elemental analyses. Compounds were tested for anticonvulsant activity utilizing pentylenetetrazole-induced seizure (PTZ) and maximal electroshock seizure (MES) tests at 30, 100 and 300 ...

The efficacy of lamotrigine and felbamate against maximal electroshock (MES)-induced seizures was assessed under conditions mimicking the pharmacoresistance associated with an increased excitatory neurotransmission. N-methyl-D-aspartate (NMDA), but not kainate applied at subconvulsive dose, reduced the activity of lamotrigine against MES-induced seizures increasing its ED50 value from 4.3 (3.2-...

Abrus precatorius which is commonly called as Indian licorice has been used for many centuries by traditional healers of Tanzania for the treatment of convulsions. The present work has been carried out to evaluate the anticonvulsant activity of the ethanolic extract (EE) of A. precatorius leaves against Pentylenetetrazole (PTZ), Picrotoxin and Maximal electroshock (MES) induced convulsions at t...

Two novel series of 3,4-dihydroisoquinolin with heterocycle derivatives (4a-t and 9a-e) were synthesized and evaluated for their anticonvulsant activity using maximal electroshock (MES) test and pentylenetetrazole (PTZ)-induced seizure test. All compounds were characterized by IR, ¹H-NMR, 13C-NMR, and mass spectral data. Among them, 9-(exyloxy)-5,6-dihydro-[1,2,4]triazolo[3,4-a]isoquinolin-3(2H...

A series of new clubbed aryl oxadiazole-1,2,4-triazine derivatives (6a-l) were designed and synthesized using appropriate chemical routes. The structures to have the required structural elements for any compounds be potential anticonvulsant. Preliminary screening anticonvulsant activity was performed maximal electroshock seizure (MES), subcutaneous pentylenetetrazole-induced (scPTZ) behavioral ...

In the recent study we have extended our investigations to the new anticonvulsant derivatives of αsubstituted N-benzylamides of γ-hydroxybutyric acid (GHB). Among the obtained compounds N-benzylamide of α-(1,2,3,4-tetrahydroisoquinoline)-GHB (9) has demonstrated activity against maximal electroshock (MES) induced seizures in mice (at 100 mg/kg ip) and in rats (at 30 mg/kg, po dose). Lactone 8 a...

The present study is an investigation of anti-epileptic activity of Malachra capitata L. (FamilyMalvaceae) is a wellknown plant which is being used in Indian traditional medicines for treating epilepsy and inflammation. The aqueous extract of Malachra capitata L. (AMC) was subjected to acute toxicity and then screened for anticonvulsant activity on Maximal Electroshock (MES) and Pentylenetetraz...

A novel series of benzenesulfonamide derivatives containing 4-aminobenzenesul-fonamide and α-amides branched valproic acid or 2,2-dimethylcyclopropanecarboxylic acid moieties were synthesized and screened for their anticonvulsant activities in mice maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) test. The activity experimental study showed that 2,2-dipropyl-N¹-(4-...

A series of novel stereochemically pure derivatives of the investigative broad-spectrum anticonvulsant ADD408003 was designed and synthesized. Five-center four-component (U-5C-4CR) and four-center three-component (U-4C-3CR) variants of Ugi reaction were used in the key step of the synthetic pathways. The compounds obtained were evaluated for the anticonvulsant activitiy in the maximal electrosh...