Abstract
A series of 2-substituted-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazoles were synthesized. The anticonvulsant effect and neurotoxicity of the compounds (intraperitoneally) were evaluated with the maximal electroshock (MES) test, subcutaneous pentylenetetrazole (sc-PTZ), and rotarod tests in mice. 2-Phenyl-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazole (3g) was the most active and also had the lowest toxicity. In the anti-MES potency test, it showed median effective dose (ED(50)) of 29.5 mg/kg, a median toxicity dose (TD(50)) of 285 mg/kg, and a protective index (PI) of 9.7, which is greater than the reference drug, carbamazepine, which has a PI of 6.4.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anticonvulsants / administration & dosage
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Anticonvulsants / chemical synthesis*
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Anticonvulsants / pharmacology*
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Anticonvulsants / toxicity
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Behavior, Animal / drug effects
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Benzoxazoles / administration & dosage
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Benzoxazoles / chemical synthesis*
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Benzoxazoles / pharmacology*
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Benzoxazoles / toxicity
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Carbamazepine / pharmacology
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Disease Models, Animal
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Electric Stimulation
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Female
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Injections, Intraperitoneal
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Magnetic Resonance Spectroscopy
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Male
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Mice
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Molecular Structure
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Motor Activity / drug effects
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Pentylenetetrazole
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Rotarod Performance Test
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Seizures / etiology
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Seizures / prevention & control*
Substances
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Anticonvulsants
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Benzoxazoles
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Carbamazepine
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Pentylenetetrazole