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Xian-Qing Deng, Li-Na Quan, Cheng-Xi Wei, and Zhe-Shan Quan.  Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives.  EUR J MED CHEM, 2011, 46:2955-63.
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Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4] triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives


×÷Õßeng, XQ (Deng, Xian-Qing)[ 1 ] ; Quan, LN (Quan, Li-Na)[ 1 ] ; Song, MX (Song, Ming-Xia)[ 1 ] ; Wei, CX (Wei, Cheng-Xi)[ 2 ] ; Quan, ZS (Quan, Zhe-Shan)[ 1 ]




EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY



¾í: 46

ÆÚ: 7

Ò³: 2955-2963

DOI: 10.1016/j.ejmech.2011.04.020

³ö°æÄê: JUL 2011

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Herein, we described the syntheses and anticonvulsant activities of 7-(substituted-phenyl)-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones (1a-1o) and their derivatives. Most of the synthesized compounds exhibited potent anticonvulsant activities in the maximal electroshock test (MES). The most promising compound 1i showed significant anticonvulsant activity in MES test with ED(50) value of 19.7 mg/kg. It displayed a wide margin of safety with protective index much higher than the standard drugs. In addition, the potence of compound 1i against seizures induced by Pentylenetetrazole, Isoniazid, Thiosemicarbazide, 3-Mercaptopropionic acid, and Bicuculline in the chemical-induced seizure tests suggested that compound 1i displayed broad spectrum activity in several models, and it is likely to have several mechanisms of action including inhibiting voltage-gated ion channels and modulating GABAergic activity. (C) 2011 Elsevier Masson SAS. All rights reserved.


¹Ø¼ü´Ê

×÷Õ߹ؼü´Ê:Synthesis; Anticonvulsant; Triazolo[1,5-a]pyrimidin; Imidazo[1,2-a]pyrimidin; Pyrazolo[1,5-a]pyrimidin; Maximal electroshock

KeyWords Plus:ANTIEPILEPTIC DRUGS; EPILEPSY; GABA; ANTAGONISM; SEIZURES; DESIGN


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ͨѶ×÷ÕßµØÖ·: Quan, ZS (ͨѶ×÷Õß)





Yanbian Univ, Coll Pharm, 977 Pk Rd, Yanji 133002, Jilin, Peoples R China.





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[ 1 ] Yanbian Univ, Coll Pharm, Yanji 133002, Jilin, Peoples R China





      

[ 2 ] Inner Mongolia Univ Nationalities, Inst Neurosurg, Tongliao 028007, Inner Mongolia, Peoples R China



µç×ÓÓʼþµØÖ·:weichengxi1224@yahoo.com.cn; zsquan@ybu.edu.cn


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National Natural Science Foundation of China


30860340

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ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 23 RUE LINOIS, 75724 PARIS, FRANCE


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Web of Science Àà±ð:Chemistry, Medicinal


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ÎÄÏ×ÀàÐÍ:Article

ÓïÖÖ:English

Èë²ØºÅ: WOS:000291895200033

ISSN: 0223-5234


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Impact Factor (Ó°ÏìÒò×Ó): Journal Citation Reports®


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