کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1397807 | 1501191 | 2010 | 7 صفحه PDF | دانلود رایگان |
A series of 9H, 10H, 3-[N- 4 methyl -2-benzamido thiophen 3-yl carbonyl amino [2-(2′-phenyl 1′- ethylenyl)] 10-(aryl) thiazolidino [4, 5-b] 1, 5 benzodiazepine [7a–7h] were designed and synthesized to meet the structural requirements essential for anticonvulsant activity. Anticonvulsant activity was determined after intra-peritoneal administration to mice by supramaximal electroshock seizures model and Isoniazide Hydrazone induced seizures model. Motor impairement was determined using actophotometer and rotarod apparatus. Among the synthesized compounds two [JG 7a and JG 7e] compounds exhibited significant anticonvulsant activity after intra-peritoneal administration. Active compounds carry hydroxy substitutent at 2-position and methoxy at 4-position in the phenyl ring at C5 of benzodiazepine. In present we study conclude that small polar and electron rich groups contribute significantly for anticonvulsant activity while electronegative substitutents showed lesser contribution for anticonvulsant activity.
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Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 3, March 2010, Pages 857–863