200875-36-1Relevant articles and documents
Synchronized Chiral Induction between [5]Helicene–Spermine Ligand and B–Z DNA Transition
Kawara, Kensuke,Tsuji, Genichiro,Taniguchi, Yosuke,Sasaki, Shigeki
, p. 1763 - 1769 (2017)
The 2,13-dimethoxy[5]helicene–spermine ligand 8 b possesses an axial chirality. The racemic 8 b was bound to B-DNA by the accompanying induction of its (P)-chirality together with the B-to-Z helicity change of the duplex DNA, [(dC-dG)3]2/
Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents
Cai, Zongyu,Deng, Liming,Geng, Xinqian,Hu, Lijun,Jiao, Shixuan,Li, Zheng,Ren, Qiang,Wang, Bin,Yang, Ying,Zhang, Luyong,Zhou, Zongtao
supporting information, (2021/12/27)
Non-alcoholic fatty liver disease (NAFLD) has become the most common hepatic disease, while no drug was approved until now. The previous study reported that the quadruple FFA1/PPAR-α/γ/δ agonist RLA8 provided better efficacy than obeticholic acid on NASH. In the present study, two design strategies were introduced to explore better quadruple FFA1/PPAR-α/γ/δ agonists with improved metabolic stability. These efforts ultimately resulted in the identification of ZLY18, a quadruple FFA1/PPAR-α/γ/δ agonist with twice higher metabolic half-life than RLA8 in the liver microsome. In the triton-1339W-induced hyperlipidemic model, ZLY18 reversed hyperlipidemia to an almost normal level, which exhibited far stronger lipid-lowering effects than that of RLA8. Moreover, ZLY18 significantly decreased steatosis, hepatocellular ballooning, inflammation and liver fibrosis in NASH model even better than RLA8. Further mechanism studies suggested that ZLY18 exerts stronger effects than RLA8 on the regulation of the gene related to lipid synthesis, oxidative stress, inflammation and fibrosis. In addition, ZLY18 is more effective than pirfenidone in the prevention of CCl4-induced liver fibrosis. Besides, ZLY18 has an acceptable safety profile in the acute toxicity study at a high dose of 500 mg/kg. Therefore, ZLY18 represents a novel and highly promising quadruple FFA1/PPAR-α/γ/δ agonist worth of further investigation and development.
PYRAZOLE-CONTAINING MACROPHAGE MIGRATION INHIBITORY FACTOR INHIBITORS
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Page/Page column 102; 103; 104, (2019/10/04)
In one aspect, the invention comprises compounds that bind and inhibit macrophage migration inhibitory factor. In another aspect, the invention provides methods of treating inflammatory disease, neurological disorders and cancer using the compounds of the invention.
Organic compound, method for preparing same, organic semiconductor material containing same, and organic transistor containing same
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Page/Page column 56, (2020/01/12)
Provided are a compound which is excellent in solubility in a solvent and easily provides a film exhibiting high mobility without complicated processes, an organic semiconductor material using the same, and an organic semiconductor ink which enables easy fabrication of an organic transistor composed of a practical configuration. The problems are solved by a method of producing a dinaphthothiophene derivative, the method including the following steps (I) and (II): (I) a first step of subjecting a naphthol derivative represented by General Formula (A) and a naphthalene thiol derivative represented by General Formula (B) to dehydration condensation in the presence of acid to produce a sulfide derivative represented by General formula (C); and (II) a second step of performing dehydrogenation reaction of the sulfide derivative (C) in the presence of a transition metal salt or a transition metal complex to produce a dinaphthothiophene derivative (D).
Optimization of Pyrazoles as Phenol Surrogates to Yield Potent Inhibitors of Macrophage Migration Inhibitory Factor
Trivedi-Parmar, Vinay,Robertson, Michael J.,Cisneros, José A.,Krimmer, Stefan G.,Jorgensen, William L.
supporting information, p. 1092 - 1097 (2018/04/30)
Macrophage migration inhibitory factor (MIF) is a proinflammatory cytokine that is implicated in the regulation of inflammation, cell proliferation, and neurological disorders. MIF is also an enzyme that functions as a keto–enol tautomerase. Most potent MIF tautomerase inhibitors incorporate a phenol, which hydrogen bonds to Asn97 in the active site. Starting from a 113-μm docking hit, we report results of structure-based and computer-aided design that have provided substituted pyrazoles as phenol alternatives with potencies of 60–70 nm. Crystal structures of complexes of MIF with the pyrazoles highlight the contributions of hydrogen bonding with Lys32 and Asn97, and aryl–aryl interactions with Tyr36, Tyr95, and Phe113 to the binding.
THERAPEUTIC PROSTAGLANDIN RECEPTOR AGONISTS
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Paragraph 0130, (2015/12/30)
Described herein are compounds which can be used in topical liquids, creams, or other dosage forms such as solids, for reducing intraocular pressure, treating glaucoma, growing hair, treating wounds, or other medical and/or cosmetic uses.
NITROGENOUS HETEROCYCLIC DERIVATIVES AND THEIR APPLICATION IN DRUGS
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Paragraph 00434, (2015/07/07)
The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, IPF, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.
Synthesis and photochromism of a spirooxazine derivative featuring a carbazole moiety: Fast thermal bleaching and excellent fatigue resistance
Zou, Qi,Li, Xin,Zhou, Ji,Bai, Kangkang,?gren, Hans
, p. 174 - 181 (2014/05/06)
A novel photochromic spirooxazine derivative bearing a carbazole moiety (SOC) was synthesized and studied in solution under flash photolysis conditions. It is found to exhibit excellent characteristics like high photochromic response, large steady-state optical density, fast thermal bleaching rate and good fatigue-resistance. The effect of different solvents on the photochromic properties of the compound was evaluated, revealing that the photochromic properties can be modulated by different solvents based on the corresponding polarity. The mechanism and kinetics of the thermal fading process of compound SOC were additionally investigated by theoretical simulations, where the isomerization pathway from the trans-trans-cis conformation was found to be several times faster than that from the cis-trans-cis conformation. This type of fast-bleaching and fatigue-resistent photochromic compounds is expected to pave an exciting avenue in future development of high-performance photochromic materials.
Indole derivatives for the treatment of depression and anxiety
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Page/Page column 14, (2010/02/05)
The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.
Piperidines derivatives and their use as serotonin receptor antagonists
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, (2010/02/05)
The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.