Abstract
New benztriazoles with a mercapto-triazole and other heterocycle substituents were synthesized and evaluated for their anticonvulsant activity and neurotoxicity by using the maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ), and rotarod neurotoxicity (TOX) tests. Among the compounds studied, compound 2-((1H-1,2,4-triazol-3-yl)thio)-N-(6-((3-fluorobenzyl)oxy)benzo[d]thiazol-2-yl)acetamide (5i) and 2-((1H-1,2,4-triazol-3-yl)thio)-N-(6-((4-fluorobenzyl)oxy)benzo[d] thiazol-2-yl)acetmide (5j) were the most potent, with an ED50 value of 50.8 mg/kg and 54.8 mg/kg in the MES test and 76.0 mg/kg and 52.8 mg/kg in the scPTZ seizures test, respectively. They also showed lower neurotoxicity and, therefore a higher protective index. In particular, compound 5j showed high protective index (PI) values of 8.96 in the MES test and 9.30 in the scPTZ test, which were better than those of the standard drugs used as positive controls in this study.
Highlights
February ninth, 2015 was the first International Epilepsy Day, and it helped more people raise awareness and understanding about epilepsy
Such efforts are urgently needed, because with more than 50 million people presenting with epilepsy worldwide, epilepsy is the most common, chronic, serious neurological disease
1H-1,2,4-triazol-3-amine (6 mmol), 2-chloro-N-(6-alkoxybenzo[d]thiazol-2-yl) acetamide (5 mmol), and sodium hydroxide (6 mmol) in N,N-dimethylformamide (10 mL) were dissolved and stirred at room temperature for 8 h. 50 mL of water was added to the reaction mixture, which was extracted with ethyl acetate (30 mL 3)
Summary
2015 was the first International Epilepsy Day, and it helped more people raise awareness and understanding about epilepsy. Such efforts are urgently needed, because with more than 50 million people presenting with epilepsy worldwide, epilepsy is the most common, chronic, serious neurological disease. 40% of patients in high-income countries and more than 70% of patients in developing countries do not get the treatment they need, because of the high expense or low availability of the appropriate drugs [1,2,3]. There is a pressing need to develop more effective antiepileptic drugs (AEDs) endowed with an improved safety profile. On the basis of a number of related materials, azoles and their derivatives have gained much attention in recent years due to their potential biological applications linked to their anticonvulsant [4], anti-inflammatory [5], anti-fungal [6], antiviral [7], and anticancer [8] activities
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