5625-08-1Relevant academic research and scientific papers
NEW ARYL-QUINOLINE DERIVATIVES
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Page/Page column 147, (2013/05/22)
The invention provides novel compounds having the general formula (I), wherein R1, R2, R3, R4 R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds.
ARYL-QUINOLINE DERIVATIVES
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Paragraph 0842; 0843, (2013/05/21)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.
Synthesis of 2-aminobenzophenone derivatives and their anticancer activity
Cortez-Maya,Cortes Cortes,Hernandez-Ortega,Apan, T. Ramirez,Martinez-Garcia
experimental part, p. 46 - 54 (2011/10/31)
A number of 2-aminobenzophenones have been synthesized by acylation of para-chloroaniline with different 2-, 3-, 4-chloro-or fluorobenzoyl chloride in solid state via the Friedel-Crafts reaction. Synthesized compounds were characterized by 1H and 13C NMR, Fourier transform-infrared, ultraviolet-visible spectroscopy, mass spectrometry, and elemental analysis. Evaluation of biological activity in vitro showed that the selected compounds 9, 10, and 13 have potential anticancer activity. The presence of one chlorine atom in the second aromatic ring of the benzophenone molecule makes it more active.
Insecticidal heterolignans-Tubuline polymerization inhibitors with activity against chewing pests
Frackenpohl, Jens,Adelt, Isabelle,Antonicek, Horst,Arnold, Christian,Behrmann, Patricia,Blaha, Nicole,Boehmer, Jutta,Gutbrod, Oliver,Hanke, Roman,Hohmann, Sabine,Houtdreve, Marc van,Loesel, Peter,Malsam, Olga,Melchers, Martin,Neufert, Valentina,Peschel, Elisabeth,Reckmann, Udo,Schenke, Thomas,Thiesen, Hans-Peter,Velten, Robert,Vogelsang, Kathrin,Weiss, Hans-Christoph
experimental part, p. 4160 - 4184 (2009/10/17)
Starting from natural product podophyllotoxin 1 substituted heterolignans were identified with promising insecticidal in vivo activity. The impact of substitution in each segment of the core structure was investigated in a detailed SAR study, and variation of substituents in both aromatic moieties afforded derivatives 5 and 43 with broad insecticidal activity against lepidopteran and coleopteran species. In vitro measurements supported by modeling studies indicate that heterolignans 3-134 act as tubuline polymerization inhibitors interacting with the colchicine-binding site. Insect specific structure-activity effects were observed showing that the insecticidal SAR described herein differs from reported cytotoxicity studies.
Sulfonyl-containing 2,3-diarylindole compounds, methods for making same, and methods of use thereof
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Page/Page column 15, (2010/02/06)
The present invention relates to sulfonyl-containing 2,3-diarylindole, especially to new compounds of general Formula, to a preparation method for their preparation, to pharmaceutical compositions containing said compound, and to the medical use thereof in the treatment of diseases relating to the inhibition of cyclooxygenase-2 (COX-2).
Synthesis and biological evaluation of substituted 2-sulfonyl-phenyl-3-phenyl-indoles: A new series of selective COX-2 inhibitors
Hu, Wenhui,Guo, Zongru,Chu, Fengming,Bai, Aiping,Yi, Xiang,Cheng, Guifang,Li, Jing
, p. 1153 - 1160 (2007/10/03)
A new series of substituted 2-sulfonyphenyl-3-phenyl-indole derivatives were synthesized and evaluated for their ability to inhibit COX-2 and COX-1enzymes. Most of the compounds synthesized were found to be highly potent and selective inhibitors of COX-2. This work led to the discovery of 2-aminosulfonylphenyl-3-phenyl-indole 5a which possesses higher activity and selectivity for COX-2 than Celecoxib both in vitro and in vivo.
