6262-27-7Relevant academic research and scientific papers
Optimization and anti-inflammatory evaluation of methyl gallate derivatives as a myeloid differentiation protein 2 inhibitor
Qiu, Yinda,Xiao, Zhongxiang,Wang, Yanyan,Zhang, Dingfang,Zhang, Wenxin,Wang, Guangbao,Chen, Wenbin,Liang, Guang,Li, Xiaokun,Zhang, Yali,Liu, Zhiguo
, (2019/08/27)
Myeloid differentiation protein 2 (MD2) is a co-receptor of toll-like receptor 4 (TLR4) responsible for the recognition of lipopolysaccharide (LPS) and mediates a series of TLR4-dependent inflammatory responses in inflammatory lung diseases including acute lung injury (ALI). Targeting MD2 thus may provide a therapeutic strategy against these lung diseases. In this study, we identified a novel compound 4k with the potent anti-inflammatory activity among 39 methyl gallate derivatives (MGDs). MGD 4k exhibited a high binding affinity to MD2, which in turn prevented the formation of the LPS/MD2/TLR4 complex. In addition, MGD 4k significantly reversed the upregulation of LPS-induced inflammatory mediators such as tumor necrosis factor-α, interleukin-6, intracellular adhesion molecule-1, vascular cell adhesion molecule-1, and monocyte chemoattractant protein-1 in vitro and in vivo. Mechanistically, MGD 4k performed anti-inflammatory function by inactivating JNK, ERK and p38 signaling pathways. Taken together, our study identified MGD 4k as a novel potential therapeutic agent for ALI through inhibiting MD2, inflammatory responses, and major inflammation-associated signaling pathways.
Methyl gallate analogue containing amide structure and application
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, (2018/12/13)
The invention discloses a methyl gallate analogue containing an amide structure and application. The structure of the methyl gallate analogue is shown as a formula (I); in the formula (I), R1 is independently selected from various alkoxy, hydroxyl, various halogens and aromatic heterocycles. The invention does a lot of experiment researches aiming at the technical field of a methyl gallate analogue which takes a hydrolyzed methyl gallate ester bond as a parent nucleus structure, and a lot of design, synthesis and pharmacological activity screening of the methyl gallate analogue which takes thehydrolyzed methyl gallate ester bond as the parent nucleus structure are carried out to obtain one type of the methyl gallate analogue which takes the hydrolyzed methyl gallate ester bond as the parent nucleus structure; the methyl gallate analogue provided by the invention has high-efficiency and broad-spectrum anti-inflammatory application. The formula I is shown in the description.
HALOGENATED BENZOTROPOLONES AS ATG4B INHIBITORS
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Page/Page column 32; 39, (2018/06/12)
The present invention relates to compounds having a benzotropolone core, and compositions containing said compounds acting as ATG4B inhibitors, thereby inhibiting autophagy. Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine, in particular for the treatment of cell proliferative disorders, such as cancer.
Inhibitory activities against topoisomerase I & II by polyhydroxybenzoyl amide derivatives and their structure-activity relationship
Abdel-Aziz, Mohamed,Matsuda, Kazuya,Otsuka, Masami,Uyeda, Masaru,Okawara, Tadashi,Suzuki, Keitarou
, p. 1669 - 1672 (2007/10/03)
o-, m-, p-Phenylenediamines having 2,3,4-trihydroxy, 3,4 dihydroxy, and 4-hydroxybenzoyl moieties were prepared and their inhibitory activities were measured against topoisomerase I and II. More hydroxy groups on two aromatic rings increased the activities. Bis(trihydroxybenzoyl)-o-phenylenediamide showed IC50=0.90 and 0.09 μM against topoisomerase I and II, respectively. Compounds with hydroxy groups protected by acetyl moiety still had the activities. Less hydroxy groups decreased their activities. Benzothiazole derivatives also indicated the activities.
