期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 7, 页码 2955-2963出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.04.020
关键词
Synthesis; Anticonvulsant; Triazolo[1,5-a]pyrimidin; Imidazo[1,2-a]pyrimidin; Pyrazolo[1,5-a]pyrimidin; Maximal electroshock
资金
- National Natural Science Foundation of China [30860340]
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.
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