25205-49-6Relevant academic research and scientific papers
Glycolytic inhibition and antidiabetic activity on synthesized flavanone scaffolds with computer aided drug designing tools
Kiruthiga, Natarajan,Saravanan, Govindaraj,Selvinthanuja, Chellappa,Sivakumar, Thangavel,Srinivasan, Kulandaivel
, p. 574 - 592 (2021/09/30)
Background: Diabetes mellitus is a challengeable metabolic disorder that leads to a group of complications when the HbA1c level is not maintained. Most of the existing drugs avail-able in the market in long-term use may lead to serious adverse effects. He
Design, synthesis and MAO inhibitory activity of 2-(arylmethylidene)-2,3-dihydro-1-benzofuran-3-one derivatives
Badavath, Vishnu Nayak,Nath, Chandrani,Ganta, Narayana Murthy,Ucar, Gulberk,Sinha, Barij Nayan,Jayaprakash, Venkatesan
, p. 1528 - 1532 (2017/07/17)
A series of 2-(arylmethylidene)-2,3-dihydro-1-benzofuran-3-one derivatives (aurones, 1–20) were synthesized and screened for their inhibitory activity against hMAO. Seventeen compounds (1–5, 7–17, 19) were found to be selective towards hMAO-B, while two w
The synthesis and synergistic antifungal effects of chalcones against drug resistant Candida albicans
Wang, Yuan-Hua,Dong, Huai-Huai,Zhao, Fei,Wang, Jie,Yan, Fang,Jiang, Yuan-Ying,Jin, Yong-Sheng
supporting information, p. 3098 - 3102 (2016/06/13)
To identify effective and low toxicity synergistic antifungal compounds, 24 derivatives of chalcone were synthesized to restore the effectiveness of fluconazole against fluconazole-resistant Candida albicans. The minimal inhibitory concentration (MIC80) and the fractional inhibitory concentration index (FICI) of the antifungal synergist fluconazole were measured against fluconazole-resistant Candida albicans. This was done via methods established by the clinical and laboratory standards institute (CLSI). Of the synthesized compounds, 2′-hydroxy-4′-methoxychalcone (8) exhibited the most potent in vitro (FICI = 0.007) effects. The structure activity relationship of the compounds are then discussed.
Design, synthesis and biological activity of flavonoid derivatives as selective agonists for neuromedin U 2 receptor
Ma, Ming-Liang,Li, Ming,Gou, Jiao-Jiao,Ruan, Tian-Yu,Jin, Hai-Shan,Zhang, Ling-Hong,Wu, Liang-Chun,Li, Xiao-Yan,Hu, Ying-He,Wen, Ke,Zhao, Zheng
, p. 6117 - 6123 (2015/02/02)
Central neuromedin U 2 receptor (NMU2R) plays important roles in the regulation of food intake and body weight. Identification of NMU2R agonists may lead to the development of pharmaceutical agents to treat obesity. Based on the structure of rutin, a typi
Total synthesis and assignment of the absolute stereochemistry of xanthoangelol J: Development of a highly efficient method for Claisen-Schmidt condensation Dedicated to Late (Dr.) Jadab C. Sarma on his 55th birthday on first May 2013
Kakati, Dwipen,Barua, Nabin C.
, p. 637 - 642 (2014/02/14)
The first total synthesis of cancer chemopreventive terpenyl hydroxychalcone xanthoangelol J isolated from Angelica keiskei was accomplished with asymmetric epoxidation, aromatic C-alkylation and Claisen-Schmidt condensation via enol mode as key steps. The crucial Claisen-Schmidt condensation has been accomplished by a novel green method using KHSO 4-SiO2 as a recyclable catalyst under microwave activation. The absolute configuration of the molecule was also determined.
The synthesis and evaluation of novel hydroxyl substituted chalcone analogs with in vitro anti-free radicals pharmacological activity and in vivo anti-oxidation activity in a free radical-injury Alzheimer's model
Pan, Ying,Chen, Yicun,Li, Qingnan,Yu, Xiaoyu,Wang, Jinzhi,Zheng, Jinhong
, p. 1693 - 1703 (2013/04/24)
Alzheimer's disease (AD) pathogenesis involves an imbalance between free radical formation and destruction. In order to obtain a novel preclinical anti-AD drug candidate, we synthesized a series of novel hydroxyl chalcone analogs which possessed anti-free radical activity, and screened their effects on scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH) and OH free radicals in vitro. Compound C7, 4,2'-dihydroxy-3,5-dimethoxychalcone was found to have potent activity in these anti-free radical activity tests. Further research revealed that C7 could elevate glutathione peroxidase (GSH-PX) and super oxide dismutase (SOD) levels and lower malonaldehyde (MDA) level in vivo in the Alzheimer's model. The indication of C7's effect on AD needs further study.
Design and synthesis of 3,5-diaryl-4,5-dihydro-1H-pyrazoles as new tyrosinase inhibitors
Zhou, Zhixuan,Zhuo, Jiaru,Yan, Sujun,Ma, Lin
, p. 2156 - 2162 (2013/05/08)
In this study, twenty 3,5-diaryl-4,5-dihydro-1H-pyrazole derivatives with hydroxyl(s) (1a-1p, 2a-2d) were synthesized and their inhibitory activity on mushroom tyrosinase was examined. The results showed that among these compounds, 1-(5-(3,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl) ethanone 1d was found to be the most potent tyrosinase inhibitor with IC 50 value of 0.301 μM. Kinetic study revealed that these compounds were competitive inhibitors of tyrosinase and their structure-activity relationships were investigated in this article.
Synthesis and evaluation of novel carbamate-substituted flavanone derivatives as potent acetylcholinesterase inhibitors and anti-amnestic agents
Anand, Preet,Singh, Baldev
, p. 1648 - 1659 (2013/07/26)
This study was designed to synthesize and evaluate flavanone derivatives with phenylcarbamate moiety as potent acetylcholinesterase (AChE) inhibitors and anti-amnestic agents for management of AD. The synthesis of carbamate-substituted flavanone derivativ
Synthesis and cdc25B inhibitory activity evaluation of chalcones
Zhao, Fei,Zhao, Qing-Jie,Zhao, Jing-Xia,Zhang, Da-Zhi,Wu, Qiu-Ye,Jin, Yong-Sheng
, p. 206 - 214 (2013/07/26)
A library of sixty-five chalcones was prepared for screening against the protein phosphatase, cdc25B. From this library, thirteen compounds were found having good inhibitory activity. Two compounds have excellent activity and can be used for the design of
