• Title/Summary/Keyword: 7-derivatives

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Chemical Constituents of Nelumbo nucifera Seeds

  • Rho, Taewoong;Yoon, Kee Dong
    • Natural Product Sciences
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    • v.23 no.4
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    • pp.253-257
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    • 2017
  • The phytochemical study for the extract of Nelumbo nucifera (Nymphaceae) seeds has led to the isolation of ten compounds including five simple phenolic compounds, two indole derivatives, a flavonoid glycoside, two abscisic acid derivatives. The interpretation of 1D and 2D NMR and ESI-Q-TOF-MS spectroscopic data revealed the chemical structures of isolates to be p-hydroxybenzoic acid (1), protocatechuic acid (2), (E)-p-coumaric acid (3), (E)-ferulic acid (4), (E)-sinapate-4-O-${\beta}$-$\text\tiny{D}$-glucopyranoside (5), tryptophan (6), 3-indoleacetic acid (7), isoschaftoside (8), dihydrophaseic acid (9), dihydrophaseic acid 3'-O-${\beta}$-$\text\tiny{D}$-glucopyranoside (10). To the best of our knowledge, 1 - 5 and 7 were identified for the first time from N. nucifera seeds, and the presence of dihydrophaseic acid (9) and its glucoside (10) were demonstrated secondly in this plant.

Electrochemical Study on the Coumarin Derivatives

  • Kim, Il Kwang;Chun, Hyun Ja;Paik, Soon Ok;Park, Sung Woo
    • Analytical Science and Technology
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    • v.8 no.4
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    • pp.655-661
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    • 1995
  • The electrochemical reduction of coumarin derivatives in 0.1M TEAP acetonitrile solution was investigated by the direct current, differential pulse polarography, cyclic voltammetry and controlled potential coulometry. The electrochemical reduction of 7-acetoxy-4-bromomethyl-coumarin(ABMC) was proceeded as an irreversible three steps(-0.58, -1.63 and -2.25 volts) of electrochemical transfer before chemical reaction. The solution color turned to yellow after the carboxyl group was reduced at 2nd step(-1.63 volts vs. Ag-AgCl) and the change in color was independant to the bromo group. Upon the basis of the results on the products analysis and the interpretaton of polarograms, a possible electrochemical reaction mechanism was suggested.

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Effects of the yaw angle on the aerodynamic behaviour of the Messina multi-box girder deck section

  • Diana, G.;Resta, F.;Zasso, A.;Belloli, M.;Rocchi, D.
    • Wind and Structures
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    • v.7 no.1
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    • pp.41-54
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    • 2004
  • An analysis refinement of the Messina Strait suspension bridge project has been recently required, concerning mainly the yaw angle effects on the multi-box deck section aerodynamics and the vortex shedding at low reduced velocities $V^*$. In particular the possible interaction of the axial flow with the large cross beams has been investigated. An original test rig has been designed at this purpose allowing for both forced motion and free motion aero elastic tests, varying the average angle of attack ${\alpha}$ and the deck yaw angle ${\beta}$. The hydraulic driven test rig allowed for both dynamic and stationary tests so that both the stationary coefficients and the flutter derivatives have been evaluated for each yaw angle. Specific free motion tests, taking advantage from the aeroelastic features of the section model, allowed also the study of the vortex shedding induced phenomena.

Synthesis and Antiinflammatory-analgesic Activity of Monovalent and Bivalent Aminoantipyrines (Monovalent와 bivalent aminoantipyrine 유도체의 합성과 항염 진통활성)

  • 김승재;권오혁;전상철;박상민;임채욱;임철부
    • YAKHAK HOEJI
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    • v.46 no.3
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    • pp.149-154
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    • 2002
  • Six novel 4-aminoantipyrine derivatives as potential nonsteroidal antiinflammatory and analgesic compounds were prepared and their antiinflammatory-analgesic activity were compared with antiprine. Succinyl chloride and Ac $_2$O were reacted with glycine, respectively, to give glycine compounds (3-4, 9-10), which were treated with hydroxysuccinimide and dicyclohexyl carbodiimide to yield active esters (5-6, 11-12), and then reacted with 4-aminoantipyrine to prepare 4-aminoantipyrine derivatives (7-8, 13-14). 4-Aminoantipyrine reacted with succinyl chloride and Ac $_2$O, respectively, to give succinyl bis aminoantipyrine (15) and acetyl aminoantipyrine (16). Compounds (7), (8) and (13) gave comparable antiinflammatory activity to antipyrine.

Design, Syntheses and Biological Evaluations of Nonpeptidic Caspase 3 Inhibitors

  • Kim, Eun-Sook;Yoo, Sung-Eun;Yi, Kyu-Yang;Lee, Sun-Kyung;Noh, Jae-Sung;Jung, Yong-Sam;Kim, Eun-Hee;Jeong, Nak-Chul
    • Bulletin of the Korean Chemical Society
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    • v.23 no.7
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    • pp.1003-1010
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    • 2002
  • Caspase 3, a member of cysteine protease family, is well known as a major apoptosis effector and is involved in cell death as a result of ischemic diseases such as stroke and myocardial infarction, therefore the inhibition of caspase 3 may protect those apoptotic cell damages. During the high-throughput screening of the compounds from the Korea Chemical Bank, berberine derivatives (A and B), an isoquinoline alkaloid, have been identified as potential inhibitors for caspase 3. Based on this finding we carried out molecular modeling study to identify the pharmacophoric elements of berberine structure which interact with a substrate-recognition binding site of caspase 3 and came up with several novel scaffolds. In this report, we will discuss the molecular modeling, syntheses and the enzyme inhibitory activities of these novel compounds.

Synthesis of 4-Phenyltetralone Derivatives and Reaction Mechanism

  • Kwon, Soon-Kyoung;Park, Young-Nam
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.329-331
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    • 2000
  • 4-(p-Chlorophenyl)tetralone (6) and 7-chloro-5-(p-chlorophenyl)tetralone (9) are key intermediates for the development of benzazepinone derivative haftens. These compounds could be synthesized from 4-phenyltetralone derivatives by triflic acid catalyzed Friedel-Crafts reaction. The reaction mechanism of Friedel-Crafts alkylation/acylation with lactones in triflic acid is presented. According to our tentative research, ring opening of protonated lactone (2) occurs in alkyl cleavage and the rate of the reaction is not dependent on concentration of triflic acid. So, alkylation of lactone in Friedel-Crafts reaction is presumed to be $A_{AL}$ 1. In second step, intramolecular acylation of the intermediates 4 to 6, 4 can be transformed to a triflic acid-carboxylic anhydride and then the cyclization is undergone after leaving of the triflate anion.

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Comparative Molecular Similarity Indices Analysis of Caspase-3 Inhibitors

  • Babu, Sathya;Madhavan, Thirumurthy
    • Journal of Integrative Natural Science
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    • v.7 no.4
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    • pp.227-233
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    • 2014
  • Caspases, a family of cysteinyl aspartate-specific proteases plays a central role in the regulation and the execution of apoptotic cell death. Activation of caspases-3 stimulates a signaling pathway that ultimately leads to the death of the cell. Hence, caspase-3 has been proven to be an effective target for reducing the amount of cellular and tissue damage. In this work, comparative molecular similarity indices analysis (CoMSIA) was performed on a series of 3,4-dihydropyrimidoindolones derivatives which are inhibitors of caspase-3. The best predictions were obtained for CoMSIA model ($q^2$ = 0.586, $r^2$ = 0.955). The predictive ability of test set ($r^2_{pred}$) was 0.723. Statistical parameters from the generated QSAR models indicated the data is well fitted and have high predictive ability. Our theoretical results could be useful to design novel and more potent caspase-3 derivatives.

Synthesis and Cytotoxicity Evaluation of Phosphorylated Derivatives of Ribavirin

  • Rao, Valasani Koteswara;Reddy, Sanapalli Subba;Babu, Kilaru Raveendra;Kumar, Kuntrapakam Hema;Ghosh, Sunil Kumar;Raju, Chamarthi Naga
    • Journal of the Korean Chemical Society
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    • v.55 no.6
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    • pp.952-959
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    • 2011
  • Novel phosphorylated derivatives of ribavirin 5-16 were synthesized by the reaction of 4-nitrophenyl phosphorodichloridate with various amino acid esters in the presence of triethylamine in dry tetrahydrofuran through the intermediates 3. On further reaction of 3 with ribavirin in THF and pyridine in the presence of TEA afforded the title compounds 5-16. Their structures were characterized by IR, $^1H$, $^{13}C$, $^{31}P$ NMR and mass spectral analyses. All the title compounds were found to exhibit potent in vitro anticancer activity against MCF-7 breast cancer cell lines.

Synthesis and SAR of Methoxyiminoacetate and Methoxyiminoacetamide Derivatives as Strobilurin Analogues

  • Hwang, In-Cheon;Kim, Joo-Kyung;Kim, Hyung-Ho;Kyung, Suk-Hun
    • Bulletin of the Korean Chemical Society
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    • v.30 no.7
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    • pp.1475-1480
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    • 2009
  • Methoxyiminoacetate and methoxyiminoacetamide derivatives possessing 2,2-dichlorovinyl side chains, have been synthesized and their biological activities against six representative plant fungal pathogens have been evaluated. Five substances in this series (3a, 4a, 3b, 3d, and 4d) were found to exhibit potent fungicidal activities compared to those of the commercially available fungicides, azoxystrobin and fenarimol.

Observer Based Nonlinear State Feedback Control of PEM Fuel Cell Systems

  • Kim, Eung-Seok
    • Journal of Electrical Engineering and Technology
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    • v.7 no.6
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    • pp.891-897
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    • 2012
  • In this paper, the observer based nonlinear state feedback controller has been developed to control the pressures of the oxygen and the hydrogen in the PEM(Proton Exchange Membrane) fuel cell system. Nonlinear model of the PEM fuel cell system was introduced to study the design problems of the state observer and model based controller. A cascade observer using the filtering technique was used to estimate the pressure derivatives of the cathode and the anode in the system. In order to estimate the pressures of the cathode and the anode, the sliding mode observer was designed by using these pressure derivatives. To estimate the oxygen pressure and the hydrogen pressure in the system, the nonlinear state observer was designed by using the cathode pressure estimates and the anode it. These results will be very useful to design the state feedback controller. The validity of the proposed observers and the controller has been investigated by using the Lyapunov's stability analysis strategy.