| Title |
Design and synthesis of chalcone derivatives as potential non-purine xanthine oxidase inhibitors
|
|---|---|
| Published in |
SpringerPlus, October 2016
|
| DOI | 10.1186/s40064-016-3485-6 |
| Pubmed ID | |
| Authors |
Trung Huu Bui, Nhan Trung Nguyen, Phu Hoang Dang, Hai Xuan Nguyen, Mai Thanh Thi Nguyen |
| Abstract |
Based on some previous research, the chalcone derivatives exhibited potent xanthine oxidase inhibitory activity, e.g. sappanchalcone (7), with IC50 value of 3.9 μM, was isolated from Caesalpinia sappan. Therefore, objectives of this research are design and synthesis of 7 and other chalcone derivatives by Claisen-Schmidt condensation and then evaluate their XO inhibitory activity. Fifteen chalcone derivatives were synthesized by Claisen-Schmidt condensation, and were evaluated for XO inhibitory activity. Nine out of 15 synthetic chalcones showed inhibitory activity (3; 5-8; 10-13). Sappanchalcone derivatives (11) (IC50, 2.5 μM) and a novel chalcone (13) (IC50, 2.4 μM) displayed strong xanthine oxidase inhibitory activity that is comparable to allopurinol (IC50, 2.5 μM). The structure-activity relationship of these chalcone derivatives was also presented. It is the first research on synthesis sappanchalcone (7) by Claisen-Schmidt condensation. The overall yield of this procedure was 6.6 %, higher than that of reported procedure (4 %). Design, synthesis, and evaluation of chalcone derivatives were carried out. This result suggests that the chalcone derivative can be used as potential non-purine XO inhibitors.Graphical abstractThe chalcone derivatives as potential non-purine xanthine oxidase inhibitors. |
Mendeley readers
The data shown below were compiled from readership statistics for 64 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 64 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Bachelor | 12 | 19% |
| Lecturer | 7 | 11% |
| Student > Ph. D. Student | 5 | 8% |
| Student > Master | 3 | 5% |
| Student > Postgraduate | 3 | 5% |
| Other | 9 | 14% |
| Unknown | 25 | 39% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 27 | 42% |
| Pharmacology, Toxicology and Pharmaceutical Science | 5 | 8% |
| Unspecified | 1 | 2% |
| Chemical Engineering | 1 | 2% |
| Nursing and Health Professions | 1 | 2% |
| Other | 3 | 5% |
| Unknown | 26 | 41% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 14 October 2016.
All research outputs
#20,346,264
of 22,893,031 outputs
Outputs from SpringerPlus
#1,460
of 1,850 outputs
Outputs of similar age
#276,486
of 319,475 outputs
Outputs of similar age from SpringerPlus
#116
of 136 outputs
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We're also able to compare this research output to 136 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.