Journal
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
Volume 21, Issue 12, Pages 1190-1204Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/10286020.2018.1529030
Keywords
1; 2; 4-triazolo[1; 5-a]pyrimidine-7(4H)-one; synthesis; anti-epileptic; molecular docking
Ask authors/readers for more resources
In this investigation, eight novel 2,5-disubstituted [1,2,4]-triazolo[1,5-a]pyrimidin-7(4H)-one and eight novel 2,5-disubstituted [1,2,4]-triazolo[1,5-a]pyrimidine amine derivatives were synthesized based on the novel marine natural product Essramycin. Their anti-epileptic activities were evaluated by 4-aminopyridine (4-AP)-induced hyper excitability model in primary cultured neocortical neurons. Five compounds with [1,2,4]-triazolo[1,5-a]pyrimidin-7(4H)-one skeleton showed remarkable anti-epileptic activities. The preliminary structure-activity relationship (SAR) showed that the pyrimidine-7(4H)-one motif is the necessary active core of anti-epileptic activity. To understand the action mechanism of anti-epileptic activity of [1,2,4]-triazolo[1,5-a]pyrimidin-7(4H)-one compounds, docking studies using the model of GABA(A) as docking scaffolds were performed and the docking results were in concordance with the experiment observations.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available