Anticonvulsant potential of certain -(6-substituted benzo[] thiazol-2-yl)-2-(4-substituted piperazin-1-yl)acetamides | ||
| Egyptian Pharmaceutical Journal | ||
| Volume 15, Issue 2, May 2016, Pages 62-69 PDF (467.3 K) | ||
| DOI: 10.4103/1687-4315.190404 | ||
| Authors | ||
| Ola Ahmed Saleh; Mohamed Farrag El-Behery; Mohamed Nabil Aboul-Enein; Aida Abd El-Sattar El-Azzouny; Yousreya Aly Maklad | ||
| Abstract | ||
| Background and objectives Epilepsy is a chronic neurological disorder. It is characterized by recurrent unprovoked occurrence of seizures that affect people of all ages. Thus, in the current work we undertook the synthesis of the joined structures of both 1, 3-benzothiazole and piperazine through amidic linkage, which will greatly foster the anticonvulsant profile of the new candidates. Experimental Synthesis of the target compounds -(6-substituted benzo[]thiazol-2-yl)-2-(4-substitued piperazinyl)acetamide derivatives () was achieved. The anticonvulsant profile of these compounds at the selected dose of 100mg/kg was investigated using maximal electroshock seizure and subcutaneous pentylenetetrazole screens as well as neurotoxicity test. Results and discussion Most of the synthesized compounds, , displayed 16.67–100% anticonvulsant activity in maximal electroshock seizure screening at a dose range of 0.22–0.31 mmol/kg. The most potent compounds were (ED=58mg/kg≡0.15 mmol/kg), (ED=64mg/kg≡0.19 mmol/kg), and (ED=60mg/kg≡0.19 mmol/kg). Compound was the only one that exhibited 100% protection in the subcutaneous pentylenetetrazole screen with ED=56mg/kg≡0.15 mmol/kg. It possessed potent activity that was about six-fold more than that of ethosuximide (ED=130mg/kg≡0.92 mmol/kg), which was used as a reference drug, and lower than that of phenobarbital (ED=13.20mg/kg≡0.06 mmol/kg). | ||
| Keywords | ||
| anticonvulsants; Benzothiazole; Epilepsy; Synthesis | ||
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