882427-72-7Relevant articles and documents
PDIA4 INHIBITORS AND USE THEREOF FOR INHIBITING ?-CELL PATHOGENESIS AND TREATING DIABETES
-
Page/Page column 17, (2021/06/11)
Disulfide-Isomerase A4 (PDIA4) inhibitors and use thereof for inhibiting pancreatic β-cell pathogenesis and treating diabetes are disclosed. Drug candidates that inhibit PDIA4 with IC50 values ranging from 4 μM to 300 nM are identified. The compounds are highly active in augmenting insulin secretion from pancreatic β-cells. The representative compound No. 8 (4,5-dimethoxy-2-propiolamidobenzoic acid), alone or in combination with metformin, is effective in preserving pancreatic β-cell function, treating and/or reversing, returning blood glucose concentration to a normal level in a diabetic.
Synthesis and evaluation of new sesamol-based phenolic acid derivatives with hypolipidemic, antioxidant, and hepatoprotective effects
Xie, Yundong,Liu, Jiping,Shi, Yongheng,Bin Wang,Wang, Xiaoping,Wang, Wei,Sun, Meng,Xu, Xinya,He, Shipeng
, p. 1688 - 1702 (2021/07/26)
The objective of this study is to synthesize a series of sesamol-based phenolic acid derivatives, which were designed by combination principle. The hypolipidemic activity of all these compounds was preliminarily screened by acute hyperlipidemic mice model induced by Triton WR 1339, in which compound T6 exhibited more significant reducing plasma TG and TC than fenofibrate. Compound T6 was also found to obviously decrease TG and TC both in the plasma and hepatic tissue of high-fat-diet-induced hyperlipidemic mice. Moreover, T6 showed hepatoprotective effects, which remarkable amelioration in characteristic liver enzymes was examined and the histopathological observation displayed that compound T6 inhibited lipids accumulation in the hepatic. The levels of PPAR-α receptor related to lipids metabolism in hepatic tissue were upregulated after T6 treatment. Other potent effects of T6 such as antioxidant and anti-inflammatory activity were also observed. On the bases of these findings, compound T6 may serve as an effective hypolipidemic and hepatoprotective agent. [Figure not available: see fulltext.]
Biological Characterization, Mechanistic Investigation and Structure-Activity Relationships of Chemically Stable TLR2 Antagonists
Bermudez, Marcel,Grabowski, Maria,Murgueitio, Manuela S.,Rademann, J?rg,Rudolf, Thomas,Tiemann, Markus,Varga, Péter,Weindl, Günther,Wolber, Gerhard
, (2020/06/08)
Toll-like receptors (TLRs) build the first barrier in the innate immune response and therefore represent promising targets for the modulation of inflammatory processes. Recently, the pyrogallol-containing TLR2 antagonists CU-CPT22 and MMG-11 were reported; however, their 1,2,3-triphenol motif renders them highly susceptible to oxidation and excludes them from use in extended experiments under aerobic conditions. Therefore, we have developed a set of novel TLR2 antagonists (1–9) based on the systematic variation of substructures, linker elements, and the hydrogen-bonding pattern of the pyrogallol precursors by using chemically robust building blocks. The novel series of chemically stable and synthetically accessible TLR2 antagonists (1–9) was pharmacologically characterized, and the potential binding modes of the active compounds were evaluated structurally. Our results provide new insights into structure-activity relationships and allow rationalization of structural binding characteristics. Moreover, they support the hypothesis that this class of TLR ligands bind solely to TLR2 and do not directly interact with TLR1 or TLR6 of the functional heterodimer. The most active compound from this series (6), is chemically stable, nontoxic, TLR2-selective, and shows a similar activity with regard to the pyrogallol starting points, thus indicating the variability of the hydrogen bonding pattern.
BIODEGRADABLE HYDROGEL AND METHODS FOR USE THEREOF
-
Paragraph 0037, (2020/06/08)
The subject matter of this invention relates to hydrogel compositions and, more particularly, to hydrogel compositions comprising block copolymers (BCPs) capable of self-assembly into nanoparticles for the delivery and controlled release of therapeutic ca
NOVEL FLUORINATED 4-ARYLOXYQUINAZOLINE DERIVATIVES AS EGFR INHIBITORS USEFUL FOR TREATING CANCERS
-
Paragraph 00112; 00114, (2019/05/02)
A novel class of fluorinated derivatives of Formula I have been prepared and found to be useful in the treatment of cancers and other EGFR related disorders. The compounds of Formula I display excellent brain penetration and an improved side effect profil
NANOPARTICLE
-
Page/Page column 23; 32-33, (2019/04/16)
The present invention relates to polycarbonate-based diblock polymers, nanoparticles comprising the diblock polymers and a therapeutic agent, in particular the therapeutic agent is attached to a magnetic moiety, and methods to prepare the diblock polymers
New uses of tetramethylpyrazine derivative in biological nerve protection
-
Paragraph 0104; 0105, (2016/10/10)
The present invention provides applications of a tetramethylpyrazine derivative having a structure represented by a formula 1, or a salt thereof, or a composition containing a tetramethylpyrazine derivative having a structure represented by the formula 1 or a salt thereof in preparation of drugs for prevention or treatment of nervous system diseases, wherein R1 is any one selected from -H, -OCH3 and -OH, R2 is any one selected from -H, -OCH3 and -OH, R3 is any one selected from -H, -OCH3, -OH and -CH3, and R4 is any one selected from -H and -OCH3. The present invention further provides a tetramethylpyrazine derivative having a structure represented by a formula 2, or a salt thereof, or a composition containing a tetramethylpyrazine derivative having a structure represented by the formula 2 or a salt thereof in preparation of drugs for prevention or treatment of nervous system diseases, wherein R1 is any one selected from -H, -OH and -OCOCH3, R2 is any one selected from -H, -OCH3 and -OH, and R3 is any one selected from -H and -OH. The formulas 1 and 2 are defined in the specification.
Caffeinated compounds and compositions for treatment of amyloid diseases and synucleinopathies
-
Page/Page column 24; 25, (2015/11/09)
Compounds and their pharmaceutically acceptable salts for treatment of β-amyloid diseases, such as observed in Alzheimer's disease and synucleinopathies, such as Parkinson's disease.
CAFFEINATED COMPOUNDS AND COMPOSITIONS FOR TREATMENT OF AMYLOID DISEASES AND SYNUCLEINOPATHIES
-
Page/Page column 35, (2013/05/21)
Compounds and their pharmaceutically acceptable salts for treatment of Beta-amyloid diseases, such as observed in Alzheimer's disease and synucleinopathies, such as Parkinson's disease
COMPOSITIONS AND METHODS FOR GLUCOSE TRANSPORT INHIBITION
-
Page/Page column 27-28, (2011/10/13)
Glucose deprivation is an attractive strategy in cancer research and treatment. Cancer cells upregulate glucose uptake and metabolism for maintaining accelerated growth and proliferation rates. Specifically blocking these processes is likely to provide new insights to the role of glucose transport and metabolism in tumorigenesis, as well as in apoptosis. As solid tumors outgrow the surrounding vasculature, they encounter microenvironments with a limited supply of nutrients leading to a glucose deprived environment in some regions of the tumor. Cancer cells living in the glucose deprived environment undergo changes to prevent glucose deprivation-induced apoptosis. Knowing how cancer cells evade apoptosis induction is also likely to yield valuable information and knowledge of how to overcome the resistance to apoptosis induction in cancer cells. Disclosed herein are novel anticancer compounds that inhibit basal glucose transport, resulting in tumor suppression and new methods for the study of glucose deprivation in animal cancer research.
