73921-19-4Relevant articles and documents
Discovery of 7-alkyloxy- [1,2,4] triazolo[1,5-a] pyrimidine derivatives as selective positive modulators of GABAA1 and GABAA4 receptors with potent antiepileptic activity
Wu, Jun,Hou, Zhipeng,Wang, Yan,Chen, Liping,Lian, Chengxi,Meng, Qingfei,Zhang, Chaoying,Li, Xiufen,Huang, Longjiang,Yu, Haibo
, (2021/12/20)
A series of 7-alkoxy - [1,2,4] triazolo [1, 5-a] pyrimidine derivatives were designed and synthesized. Maximal electroshock (MES) and pentylenetetrazole (PTZ) tests were utilized to access their anticonvulsant activity. Most of the series of compounds exhibited significant anti-seizure effects. Further studies demonstrated that the anticonvulsant activity of these compounds mainly depended on their allosteric potentiation of GABAA receptors. Among them, compound 10c was picked for the mechanism study due to its potent activity. The compound is more sensitive to subunit configurations of synaptic α1β2γ2 and extrasynaptic α4β3δ GABAA receptors, but there were no effects on NMDA receptors and Nav1.2 sodium channels. Meanwhile, 10c acted on the sites of GABAA receptors distinct from commonly used anticonvulsants benzodiazepines and barbiturates. Furthermore, studies from native neurons demonstrated that compound 10c also potentiated the activity of native GABAA receptors and reduced action potential firings in cultured cortical neurons. Such structural compounds may lay a foundation for further designing novel antiepileptic molecules.
5 - N-propyl -4 -hydroxypyrrole -2 - ketone derivative as well as preparation method and application thereof
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Paragraph 0052; 0059-0060, (2021/11/03)
5 - N-propyl -4 -hydroxypyrro -2 -one derivatives as well as a preparation method and application thereof are disclosed. The 5 -n-propyl -4 -hydroxypyrrole -2 - ketone derivative provided by the invention has a significant improvement in weeding activity
Ruthenium-catalyzed intramolecular cyclization of diazo-β-ketoanilides for the synthesis of 3-alkylideneoxindoles
Chan, Wai-Wing,Kwong, Tsz-Lung,Yu, Wing-Yiu
experimental part, p. 3749 - 3755 (2012/06/01)
With [Ru(p-cymene)Cl2]2 as catalyst, diazo-β-ketoanilides would undergo intramolecular carbenoid arene C-H bond functionalization to afford 3-alkylideneoxindoles in up to 92% yields. The reaction occurs under mild conditions and exhibits excellent chemoselectivity. The lack of primary KIE (kH/kD ~ 1) suggests that the reaction should not proceed by rate-limiting C-H bond cleavage; a mechanism involving cyclopropanation of the arene is proposed.