96155-82-7Relevant academic research and scientific papers
AMINE OR (THIO)AMIDE CONTAINING LXR MODULATORS
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Page/Page column 113, (2019/02/06)
The present invention relates to derivatives of formula (I) which bind to the liver X receptor (LXRα and/or LXRβ) and act preferably as inverse agonists of LXR.
Endothelin antagonists benzene oxygen benzene acetic acids and its preparation method and application
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Paragraph 0056-0057, (2016/11/02)
The invention provides a phenoxy phenylacetic acid endothelin antagonist shown in a formula (I) or a pharmaceutically acceptable salt thereof, and also provides a preparation method of the benzene oxygen phenylacetic acid endothelin antagonist or the pharmaceutically acceptable salt thereof, and an application thereof in preparation of a medicament for treating cardiovascular and cerebrovascular diseases, tumors, diabetes mellitus, nephrosis, asthma or hyperthyroidism.
Synthesis and PGE2 production inhibition of s-triazine derivatives as a novel scaffold in RAW 264.7 macrophage cells
Kang, Seoung Mook,Lee, Jinsung,Jin, Jae Ho,Kim, Minju,Lee, Sunhoe,Lee, Hwi Ho,Shin, Ji-Sun,Lee, Kyung-Tae,Lee, Jae Yeol
, p. 5418 - 5422 (2015/01/08)
We present the synthesis and biological evaluation of a collection of s-triazine derivatives as a novel scaffold of compounds with the capability to inhibit the PGE2 production in LPS-induced RAW 264.7 macrophage cells. A total of 12 derivatives were synthesized and assayed for PGE2 reduction at 10 μM concentration. Two compounds (7b and 7i) exhibiting >90% inhibition of PGE2 production were found to have IC50 values of 5.76 and 5.52 μM, respectively. They were counter screened for inhibition on COX-2 activity in a cell free assay. Specifically, compound 7i (R1 = 4-Bn-Ph, R2 = Cl, R3 = Ph, R5 = CO2Me) was highly active in cells while maintaining little COX-2 inhibition (~0% at 10 μM). Molecular docking study provides the possibility that compound 7i could inhibit PGE2 production by blocking the PGH2 binding site of mPGES-1 instead of COX-2 enzyme. Based on this result, our synthetic efforts will focus on intensive structure-activity relationship (SAR) study of s-triazine scaffold to discovery a potential PGE2 synthesis inhibitor.
Synthesis of α,α-disubstituted α-amino esters: Nucleophilic addition to iminium salts generated from amino ketene silyl acetals
Hata, Shingo,Koyama, Hiroshi,Shimizu, Makoto
experimental part, p. 9670 - 9677 (2012/01/04)
Alkoxycarbonyl iminium species are prepared easily by the oxidation of tetrasubstituted amino ketene silyl acetals, and subsequent nucleophilic addition of Grignard reagents to the iminium salts gives α,α- disubstituted α-amino ester derivatives in moderate to good yields, in which aryl and ethynyl substituents are readily introduced.
Generation of iminyl copper species from α-azido carbonyl compounds and their catalytic C-C bond cleavage under an oxygen atmosphere
Chiba, Shunsuke,Zhang, Line,Ang, Gim Yean,Hui, Benjamin Wei-Qiang
supporting information; experimental part, p. 2052 - 2055 (2010/07/04)
Figure presented A copper-catalyzed reaction of α-azidocarbonyl compounds under an oxygen atmosphere is reported where nitriles are formed via C-C bond cleavage of a transient iminyl copper intermediate. The transformation is carried out by a sequence of denitrogenative formation of iminyl copper species from α-azidocarbonyl compounds and their C-C bond cleavage, where molecular oxygen (1 atm) is a prerequisite to achieve the catalytic process and one of the oxygen atoms of O2 was found to be incorporated into the β-carbon fragment as a carboxylic acid.
α-alkyl substituted pirinixic acid derivatives as potent dual agonists of the peroxisome proliferator activated receptor alpha and gamma
Rau, Oliver,Syha, Yvonne,Zettl, Heiko,Kock, Michael,Bock, Andreas,Schubert-Zsilavecz, Manfred
experimental part, p. 191 - 195 (2009/04/04)
Peroxisome proliferator-activated receptors (PPAR) are nuclear receptors, playing a pivotal role in energy homeostasis. Activators of the PPARα subtype are in widespread use for the treatment of hyperlipidemia, while activators of the PPARγ subtype are in clinical use for the treatment of type-2 diabetes. Since both of these diseases are frequently associated, the combined treatment with one drug simultaneously activating PPARα and PPARγ seems worthwhile. Starting with pirinixic acid, which is a moderately active dual PPARα/γ agonist, we improved potency at the human PPARα and PPARγ by substituting the a-position with an aliphatic chain. The maximal effect was achieved at a chain length of four and six carbons, respectively, leading to an activity induction by a factor of 36 for PPARα and 18 for PPARγ, respectively.
Growth hormone secretagogues
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Page column 41, (2010/02/09)
What is disclosed are growth hormone secretagogues, and their uses, of the formula wherein R1 is C6H5CH2OCH2—, C6H5(CH2)3— or indol-3-ylmethyl; Y is pyrrolidin-1-yl, 4-C1-C6alkylpiperidin-1-yl or NR2R2; R2 are each independently a C1to C6alkyl; R3 is 2-napthyl or phenyl para-substituted by W; W is H, F, CF3, C1-C6alkoxy or phenyl; and R4 is H or CH3, or a pharmaceutically acceptable salt or solvate thereof.
Electrolytic partial fluorination of organic compounds: Part 25. Regioselective anodic fluorination of naphthalene- and pyridine-acetate and -acetonitrile derivatives
Higashiya, Seiichiro,Sato, Takayuki,Fuchigami, Toshio
, p. 203 - 208 (2007/10/03)
Anodic regioselective fluorination of α-phenylsulphenylated ethyl acetates and acetonitriles of 1-naphthalene and 2-pyridine derivatives was investigated. 1-Naphthalene derivatives were selectively fluorinated at the α-carbon using Et3N · 3HF/C
ANGIOTENSIN II ANTAGONISTS INCORPORATING A SUBSTITUTED PYRIDOIMIDAZOLYL RING
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, (2008/06/13)
Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists. STR1
Cathodic Reduction of Ethyl α-Bromonaphthalene-1- and-2-acetate: Electrochemical Synthesis and Voltammetric Behaviour of meso- and DL-Diethyl 2,3-Di-1- and-2-naphthylsuccinate
De Luca, Carlo,Inesi, Achille,Rampazzo, Liliana
, p. 209 - 212 (2007/10/02)
Diethyl 2,3-dinaphthylsuccinates (5)-(8) can be prepared through electrochemical reduction of ethyl α-bromonaphthalene-1- and -2-acetate (3) or (4) (ABr) in DMF-0.1 M Et4NClO4 at a vitreous carbon electrode.These dinaphthylsuccinates (5)-(8) (A-A) are good model systems for the study of electron transfer to molecules containing two identical redox centres.Cyclic voltammetry shows that dimeric species A-A are reduced at more positive potentials than the corresponding AH compound; meso-diethyl 2,3-di-2-naphthylsuccinate (7) is reduced at a slightly more positive potential than the corresponding DL-succinate (8).The 1-naphthyl derivatives are more easily reduced than the corresponding 2-naphthyl compounds, the difference being larger between bromoesters (3) and (4).
