55882-65-0Relevant academic research and scientific papers
A Series of Ferulic Acid Amides Reveals Unexpected Peroxiredoxin 1 Inhibitory Activity with in vivo Antidiabetic and Hypolipidemic Effects
Yasmin, Sabina,Cerchia, Carmen,Badavath, Vishnu Nayak,Laghezza, Antonio,Dal Piaz, Fabrizio,Mondal, Susanta K.,Atl?, ?zlem,Baysal, Merve,Vadivelan, Sankaran,Shankar,Siddique, Mohd Usman Mohd,Pattnaik, Ashok Kumar,Singh, Ravi Pratap,Loiodice, Fulvio,Jayaprakash, Venkatesan,Lavecchia, Antonio
, p. 484 - 498 (2020/11/02)
Insulin resistance is a major pathophysiological feature in the development of type 2 diabetes (T2DM). Ferulic acid is known for attenuating the insulin resistance and reducing the blood glucose in T2DM rats. In this work, we designed and synthesized a library of new ferulic acid amides (FAA), which could be considered as ring opening derivatives of the antidiabetic PPARγ agonists Thiazolidinediones (TZDs). However, since these compounds displayed weak PPAR transactivation capacity, we employed a proteomics approach to unravel their molecular target(s) and identified the peroxiredoxin 1 (PRDX1) as a direct binding target of FAAs. Interestingly, PRDX1, a protein with antioxidant and chaperone activity, has been implied in the development of T2DM by inducing hepatic insulin resistance. SPR, mass spectrometry-based studies, docking experiments and in vitro inhibition assay confirmed that compounds VIe and VIf bound PRDX1 and induced a dose-dependent inhibition. Furthermore, VIe and VIf significantly improved hyperglycemia and hyperlipidemia in streptozotocin-nicotinamide (STZ-NA)-induced diabetic rats as confirmed by histopathological examinations. These results provide guidance for developing the current FAAs as new potential antidiabetic agents.
Design, synthesis, and bioassay of 4-thiazolinone derivatives as influenza neuraminidase inhibitors
Xiao, Mengwu,Xu, Lvjie,Lin, Ding,Lian, Wenwen,Cui, Manying,Zhang, Meng,Yan, Xiaowei,Li, Shuishi,Zhao, Jun,Ye, Jiao,Liu, Ailin,Hu, Aixi
, (2021/02/09)
A series of 4-thiazolinone derivatives (D1-D58) were designed and synthesized. All of the derivatives were evaluated in vitro for neuraminidase (NA) inhibitory activities against influenza virus A (H1N1), and the inhibitory activities of the five most pot
Ferulic acid amide derivative, and synthesis method and application thereof
-
Paragraph 0022-0024, (2021/06/13)
The invention provides a ferulic acid amide derivative represented by the following general formula IV, wherein R represents phenyl, p-methoxyphenyl, 4-aminodiphenyl ether, 4-trifluoromethoxyphenyl, 4-(trifluoromethyl)phenyl, 3-aminobenzene isopropyl ethe
Thiourea derivatives, and preparation method and application thereof
-
Paragraph 0042-0045, (2020/06/05)
The invention relates to thiourea derivatives represented by formula I, pharmaceutically acceptable salts thereof and a pharmaceutical composition thereof, and an application of the thiourea derivatives in the preparation of an influenza virus neuraminida
Construction of 3D Antioxidants with Nucleosides as the Core: Inhibition of DNA Oxidation
Zhao, Peng-Fei,Liu, An,Wei, Ming-Guang,Liu, Zai-Qun
, p. 15854 - 15864 (2019/12/25)
We herein attach ferulic and caffeic acids to -OH and -NH2 in cytidine, uridine, adenosine, or guanosine for achieving antioxidative hybrids with three-dimensional (3D) configuration. In the case of molecular docking computation, the nucleoside
Regioselective synthesis of 7-O-esters of the flavonolignan silibinin and SARs lead to compounds with overadditive neuroprotective effects
Schramm, Simon,Huang, Guozheng,Gunesch, Sandra,Lang, Florian,Roa, Judit,H?gger, Petra,Sabaté, Raimon,Maher, Pamela,Decker, Michael
supporting information, p. 93 - 107 (2018/02/15)
A series of neuroprotective hybrid compounds was synthesized by conjugation of the flavonolignan silibinin with natural phenolic acids, such as ferulic, cinnamic and syringic acid. Selective 7-O-esterfication without protection groups was achieved by appl
Preparation of ferulic acid dimer derivative and application of ferulic acid dimer derivative to treatment of Alzheimer's disease
-
Paragraph 0020; 0021; 0026; 0027; 0028, (2018/07/30)
The invention discloses a ferulic acid dimer derivative and a preparation method thereof. Modification is carried out on the structural foundation of a natural lead compound ferulic acid; the preparedferulic acid derivative keeps the capability of elimina
Study on the anticoagulant or procoagulant activities of type II phenolic acid derivatives
Luo, Xuan,Du, Chuanrong,Cheng, Hui,Chen, Jian-hua,Lin, Cuiwu
, (2017/12/05)
In this study, three type II phenolic acids (caffeic acid, p-hydroxycinnamic acid, and ferulic acid) were used to synthesize a total of 18 phenolic acid derivatives. With molecular docking for molecule design and target protein (factors) screening, in combination with the confirmation of target proteins (factors) by surface plasmon resonance, and the evaluation of haemostatic and anticoagulant activities with five blood assays (plasma recalcification time, prothrombin time, activated partial thromboplastin time, fibrinogen, and thrombin time), the data indicated that caffeic acid derivatives showed certain anticoagulant or procoagulant activities and that two other series contained compounds with the best anticoagulant activities. Using Materials Studio analysis, particular functional groups that affect anticoagulant or procoagulant activities were revealed, and these conclusions can guide the discovery of compounds with better activities.
Monoamine Oxidase Inhibitory Activity of Ferulic Acid Amides: Curcumin-Based Design and Synthesis
Badavath, Vishnu N.,Baysal, Ipek,Uar, Gülberk,Mondal, Susanta K.,Sinha, Barij N.,Jayaprakash, Venkatesan
, p. 9 - 19 (2016/01/29)
Ferulic acid has structural similarity with curcumin which is being reported for its monoamine oxidase (MAO) inhibitory activity. Based on this similarity, we designed a series of ferulic acid amides 6a-m and tested for their inhibitory activity on human MAO (hMAO) isoforms. All the compounds were found to inhibit the hMAO isoforms either selectively or non-selectively. Nine compounds (6a, 6b, 6g-m) were found to inhibit hMAO-B selectively, whereas the other four (6c-f) were found to be non-selective. There is a gradual shift from hMAO-B selectivity (6a,b) to non-selectivity (6c-f) as there is an increase in chain length at the amino terminus. In case of compounds having an aromatic nucleus at the amino terminus, increasing the carbon number between N and the aromatic ring increases the potency as well as selectivity toward hMAO-B. Compounds 6f, 6j, and 6k were subjected to membrane permeability and metabolic stability studies by in vitro assay methods. They were found to have a better pharmacokinetic profile than curcumin, ferulic acid, and selegiline. In order to understand the structural features responsible for the potency and selectivity of 6k, we carried out a molecular docking simulation study.
NOVEL KOJIC ACID CONJUGATED COMPOUNDS AND THEIR BIOLOGICAL APPLICATIONS
-
Paragraph 0151-0154, (2016/10/10)
The present invention relates to a novel kojic acid conjugated compound conjugated by a click reaction of kojic acid and an antioxidant derivative, an antioxidant dietary supplement comprising the same, and a composition for external application on skin h
