13 research outputs found
Experimental Pharmacology: Increased Aspartate Release from Brain Slices of Epileptic Experimental Animals and Effect of Valproate on It
Idiopathic cardiac asystole presenting as an intractable adult onset partial seizure disorder
Lipid Peroxidation and the Antioxidant Effects of 3,5,7,4'-Tetrahydroxy-2'-Methoxyflavone; Direct Observation by Atomic Force Microscopy.
Late seizures in patients with internal carotid and middle cerebral artery occlusive disease following ischaemic events.
Role of heme oxygenase in heme-mediated inhibition of rat brain Na+?K+-ATPase: Protection by tin-protoporphyrin
Microwave-assisted synthesis, anticonvulsant activity and quantum mechanical modelling of N-(4-bromo-3-methylphenyl) semicarbazones
Objective: To study the effect of halo substitution on disubstituted aryl semicarbazones on the anticonvulsant potential and model the activity based on quantum mechanics. Methods: A series of twenty-six compounds of N(4)-(4-bromo-3-methylphenyl) semicarbazones were synthesized and evaluated for the anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure threshold tests. Some potential compounds were also tested in the subcutaneous strychnine (scSTY) and subcutaneous picrotoxin (scPIC) seizure threshold tests. The synthesized compounds were tested for behavioral impairment and CNS (central nervous system) depression in mice. Quantum mechanical modelling was carried out on these compounds to gain understanding on the structural features essential for activity. Results: Some compounds possessed broad spectrum anticonvulsant activity as indicated by their effect in pentylenetetrazole, strychnine, picrotoxin and maximal electroshock seizures models in resemblance to other aryl semicarbazone derivatives reported earlier. The higher the difference in HOMO (highest occupied molecular orbital) and LUMO (lowest unoccupied molecular orbital) energy levels was, the greater was the activity profile. Conclusion: The pharmacophoric requirements for compounds to exhibit anticonvulsant activity that includes one aryl unit in proximity to a hydrogen donor-acceptor domain and an electron donor have been justified with the molecular orbital surface analysis of the synthesized compounds