128837-26-3Relevant articles and documents
Synthetic method of 1,3-substituted Diphenylpropenes
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Paragraph 0019-0020; 0022, (2017/07/19)
The present invention relates to a method for efficiently synthesizing a natural 1,3-substituted diphenylpropene compound having biological activity. The effective method synthesizes 1,3-substituted diphenylpropene compound 1 to 4 using Friedel-Crafts alk
Synthetic method for aurone compounds and anti-inflammatory compounds containing thereof
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Paragraph 0062-0063, (2017/10/21)
The present invention relates to a synthesis method capable of synthesizing aurone compounds, Rreogoron A (Compound 1a), Gram-flavonoid A (Compound 1b), and derivatives thereof (Compounds 1c to 1o) in a high yield from the disclosed commercially-available products. Also, their anti-inflammatory effects were evaluated in LPS-induced RAW-264.7 macrophages. The aurone compounds do not show cytotoxicity, and weakens or reduces the generation of nitrogen oxide that is induced by LPS at 10 andmu;M, and the IC_50 values of the compounds 1a - 1o are each in the range of 3.39-19.55 andmu;M. Among 15 aurone compounds synthesized in the present invention, the highest inhibitory activities were shown by the following compounds in this order: the compound 1g (63.98%; IC_50= 4.50), the compound 1o (49.07%; IC_50= 4.98) and the Rreogoron A (41.72%; IC_50= 3.39). Among the aurone compounds derived from 5,6-dimethoxybenzofuran-3(2H)-one (Compound 5), the compounds bound to 4-bromophenyl group (Compound 1g), ferrocenyl group (Compound 1o), and 4-hydroxyphenyl group (Compound 1a) were more effective to iNOS-mediated nitrogen oxide inhibitors than other aurone compounds.COPYRIGHT KIPO 2017
Facile synthesis and nitric oxide inhibitory activity of aurones, rugaurone a, gramflavonoid a and their derivatives
Damodar, Kongara,Kim, Jin-Kyung,Jun, Jong-Gab
, p. 1091 - 1098 (2016/11/25)
Facile synthesis of natural aurones, rugaurone A (1a), gramflavonoid A (1b) and their novel derivatives (1c-1o) is accomplished in good to high yields with exceptional Z-selectivity (≥ 97%) from the commercially available starting materials. Herein, practically improved method was developed for the synthesis of common key intermediate, 5,6-dimethoxybenzofuran-3(2H)-one (5). Later, their nitric oxide (NO) production inhibition effects were estimated in lipopolysaccharide (LPS)-induced RAW-264.7 macrophages as an indicator of anti-inflammatory activity. All compounds exhibited weak to good strength against NO production in a concentration-dependent manner and none of the compound showed significant cytotoxicity against macrophages at the highest (10 μM) concentration. The IC50 values are showed in the range from 3.39 to 19.55 μM. Among the 15 aurones synthesized in this study, 3 compounds that is compound 1g (63.98%) followed by compound 1o (49.07%) and rugaurone A (1a) (41.72%) showed the maximum inhibitory activity with respective IC50 values of 4.50 μM, 4.98 μM and 3.39 μM compared to L-NMMA (IC50 = 5.19 μM), which was used as a standard NO inhibitor. This study suggests that compounds 1g, 1o and 1a may serve as favorable structures for further development of NO production-targeted anti-inflammatory agents.
Syntheses and anti-inflammatory activity of natural 1,3-diarylpropenes
Jung, Jong-Woon,Kim, Jin-Kyung,Jun, Jong-Gab
, p. 632 - 637 (2016/06/09)
First syntheses of five natural 1,3-diarylpropenes (cinnamylphenols) 2-4, 7, and 8 along with synthesis of two other natural 1,3-diarylpropenes 1 and 5 and E-isomer of mucronulastyrene (6) were achieved by Friedel- Crafts alkylation as a key step. Subsequ
Peptide analogues comprising at least one type of aminoacylaza-γ(b)3and the use thereof, in particular for therapy
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, (2011/04/14)
The object of the present invention is analogues of peptides or parent proteins, these peptide analogues, comprising at least one aza-β3 aminoacyl residue, and also their uses in pharmaceutical compositions or for the diagnosis of pathologies w
Directed lithiation in arenetricarbonylchromium(0) complexes: Assessment of some directing group specificities and of electrophilic quench efficacies
Sebhat, Iyassu K.,Tan, Yen-Ling,Widdowson, David A.,Wilhelm, René,White, Andrew J.P.,Williams, David J.
, p. 6121 - 6134 (2007/10/03)
The synthesis of a series of phenol ethers and 4-triisopropylsilyloxymethylphenol ethers and their η6-tricarbonylchromium(0) complexes are reported. The directed lithiation of these followed by quenching with a series of electrophiles gave acce
Syntheses of natural 4,4'-dihydroxy-2',6'-dimethoxy- and 4,2'-dihydroxy-4',6'-dimethoxy-3'-(γ,γ-dimethylallyl)-chalcones
Jain, A. C.,Sinha, S. P.
, p. 317 - 320 (2007/10/02)
The natural chalocone 6 has been synthesised from 6-O-methylphloroacetophenone (1) by ethoxymethylation, methylation, condensation with 4-ethoxymethoxybenzaldehyde (4) and finally deethoxymethylation with 4percent methanol
