1218940-40-9Relevant academic research and scientific papers
Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4] triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives
Deng, Xian-Qing,Quan, Li-Na,Song, Ming-Xia,Wei, Cheng-Xi,Quan, Zhe-Shan
experimental part, p. 2955 - 2963 (2011/06/27)
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 ED50 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.
Three-component synthesis of 4-aryl-1H-pyrimido[1,2-a] benzimidazole derivatives in ionic liquid
Yao, Changsheng,Lei, Song,Wang, Cuihua,Li, Tuanjie,Yu, Chenxia,Wang, Xiangshan,Tu, Shujiang
experimental part, p. 26 - 32 (2010/05/03)
(Chemical Equation Presented) A green and simple synthesis of 4-ayrl-3,4-dihydro-1H-pyrimido[1,2-a]benzimidazole derivatives was accomplished in excellent yields via the reaction of aryl aldehyde, 1,3-dicarbonyl compounds and 1Hbenzo[ d]imidazol-2-amine in ionic liquid of [bmim+][BF 4- ]. This protocol has the advantages of easier work-up, mild reaction conditions, high yields, and an environmentally benign procedure compared with the reported methods.
