A series novel of N-(2-hydroxyethyl)amide derivatives was synthesized and screened for their anticonvulsant activities by the maximal electroshock (MES) test, and their neurotoxicity was evaluated by the rotarod test (Tox). The maximal electroshock test showed that N-(2-hydroxyethyl)decanamide 1g, N-(2-hydroxyethyl)palmitamide 1l, and N-(2-hydroxyeth-yl)stearamide 1n were found to show a better anticonvulsant activity and also had lower toxicity than the marked anti-epileptic drug valproate. In the anti-MES potency test, these compounds exhibited median effective doses (ED50) of 22.0, 23.3, 20.5 mg/kg, respectively, and median toxicity doses (TD50) of 599.8, >1000, >1000 mg/kg, respectively, resulting in a protective index (PI) of 27.5, >42.9, >48.8, respectively. This is a much better protective index than that of the marked anti-epileptic drug valproate (PI = 1.6). To further investigate the effects of the anticonvulsant activity in several different models, compounds 1g, 1l, and 1n were tested having evoked convulsions with chemical substances, including pentylenetetrazloe, isoniazide, 3-mercaptopropionic acid, bicuculline, thiosemicarbazide, and strychnine.
Anticonvulsant activity X 0190 Synthesis and Anticonvulsant Activity of N-(2-Hydroxyethyl)amide Derivatives. -19 Title compounds of type (I) are prepared and screened for their anticonvulsant activities by the maximal electroshock (MES) test. The derivatives (I) show a better anticonvulsant activity and a lower toxicity than the anti-epileptic drug valproate. -(GUAN, L.-P.; ZHAO, D.-H.; XIU, J.-H.; SUI, X.; PIAO, H.-R.; QUAN*
In order to explore the educational model of combined research aidding basic medical education and clinical practice, the educational form of combined research, teaching and clinical practice was adopted and brought into the education of medical genetics for medical students. The consequence of five-year educational practice has revealed that the educational effects and quality have been obviously increased, and the deeply activated studying initiative, self-studying ability, ability of cooperation, discovering and creative ability have been achieved in culturing practical general medical students with in-depth basic knowledge, great ability and high quality.
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