ORIGINAL ARTICLE
Year : 2016  |  Volume : 15  |  Issue : 2  |  Page : 62-69

Anticonvulsant potential of certain N-(6-substituted benzo[d] thiazol-2-yl)-2-(4-substituted piperazin-1-yl)acetamides


1 Pharmaceutical Chemistry Group, Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre (ID: 60014618), 33 El bohouth Street, Dokki-Giza, Egypt
2 Pharmacology Group, Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre (ID: 60014618), 33 El bohouth Street, Dokki-Giza, Egypt

Correspondence Address:
Mohamed Nabil Aboul-Enein
Pharmaceutical Chemistry Group, Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre (ID: 60014618), 33 El bohouth Street, Dokki-Giza
Egypt
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/1687-4315.190404

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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 N-(6-substituted benzo[d]thiazol-2-yl)-2-(4-substitued piperazinyl)acetamide derivatives (4a–f) was achieved. The anticonvulsant profile of these compounds at the selected dose of 100 mg/kg was investigated using maximal electroshock seizure and subcutaneous pentylenetetrazole screens as well as neurotoxicity test. Results and discussion Most of the synthesized compounds, 4a–f, 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 4a (ED50 = 58 mg/kg≡0.15 mmol/kg), 4b (ED50 = 64 mg/kg≡0.19 mmol/kg), and 4c (ED50 = 60 mg/kg≡0.19 mmol/kg). Compound 4a was the only one that exhibited 100% protection in the subcutaneous pentylenetetrazole screen with ED50 = 56 mg/kg≡0.15 mmol/kg. It possessed potent activity that was about six-fold more than that of ethosuximide (ED50 = 130 mg/kg≡0.92 mmol/kg), which was used as a reference drug, and lower than that of phenobarbital (ED50 = 13.20 mg/kg≡0.06 mmol/kg).


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