• Biomolecules & Therapeutics
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• v.8 no.4
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• pp.349-353
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• 2000

Mefenamic acid has been widely used as clinical drug for anti-inflammatory and analgesic. This drug was known to non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen and indomethacin. Although the drugs which comprise this group are of diverse chemical structures, they all share the antipyretic, analgesic and anti-inflammatory actions which are characteristic of aspirin. Action of this drugs is caused by inhibitory effect of biosynthesis of prostaglandin that are synthesized from arachidonic acid via the endoperoxide biosynthesis pathway, the initial step of which is catalysed by cyclooxygenase. Mefenamic acid has more potent inhibitory action of prostaglandin biosynthesis than aspirin. Therefore, mefenamic acid is expected to have anticoagulant activity as aspirin-like drugs. This study was carried out to investigate the sinthesis of mefenamic acid derivatives from mefenamic acid and aromatic compound of antioxidant and its antioxidative and anticoagulant activities. Synthesis of mefenamic acid derivatives was conformed by conjugation as using esterification method. Biological activities was examined using effect of anticoagulant on bleeding time and effect of antioxidant by TBA method. As a result, SJ-202 showed strong antioxidative activity and anticoagulant activity among tested 4 compounds and exhibited similar activity to aspirin at anticoagulant activity.

• Applied Chemistry for Engineering
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• v.17 no.3
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• pp.286-290
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• 2006

New quaternary ammonium chlorides, [alkyldimethyl-[5-(2-phenylthiazol-4-yl]-1,3,4-oxadizol-2-ylmethyl]quaternary ammonium chlorides (ADOQACs): 6] were obtained with high yields by the reaction of compound 5 with N,N-dimethylalkyl amines in isopropyl alcohol. The structures and physical properties of the synthesized compounds were investigated and those surface-active properties were measured. The surface tension ($\gamma_{cmc}$) and the minimal inhibitory concentration (MIC) of compound 6 were found to be influenced by the number of alkyl chain carbon. Especially, compounds 6c and 6d exhibited high anti-bacterial activities and good surface-active properties.

• Food Science and Biotechnology
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• v.16 no.6
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• pp.1060-1063
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• 2007

The antioxidative activity of Alpinia oxyphylla was investigated through measuring the radical scavenging effect on 1,1-diphenyl-2-picrylhydrazyl (DPPH) and inhibitory activity for linoleic acid peroxidation. Two antioxidative diarylheptanoids, yakuchinone A (1) and oxyphyllacinol (2), were isolated from the fruits of A. oxyphylla using thin layer chromatography (TLC) autographic assays. The DPPH scavenging activities of the compounds ($IC_{50}=1$, $57{\pm}2.1\;{\mu}M$; 2, $89{\pm}3.1\;{\mu}M$) were lower than vitamin C ($IC_{50}=51{\pm}1.1\;{\mu}M$), but higher than butylated hydroxytoluene (BHT, $IC_{50}=99{\pm}2.2\;{\mu}M$). Also, inhibitory activities for linoleic acid peroxidation of the compounds ($IC_{50}=1$, $0.19{\pm}0.011\;mM$; 2, $0.31{\pm}0.009\;mM$) were higher than those of vitamin C ($IC_{50}=0.59{\pm}0.017\;mM$) and BHT ($IC_{50}=0.52{\pm}0.014\;mM$). In addition the $^{13}C-NMR$ data of oxyphyllacinol (2) have been first reported in this paper.

• Journal of Microbiology and Biotechnology
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• v.23 no.3
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• pp.329-334
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• 2013

Uridinediphospho-N-acetylglucosamine enolpyruvyl transferase (MurA, E.C. 2.5.1.7) is an essential bacterial enzyme that catalyzes the first step of the cell wall biosynthetic pathway, which involves the transfer of an enolpyruvyl group from phosphoenolpyruvate to uridinediphospho-Nacetylglucosamine. In this study, novel inhibitors of Haemophilus influenzae MurA (Hi MurA) were identified using high-throughput screening of a chemical library from the Korea Chemical Bank. The identified compounds contain a quinoline moiety and have much lower effective inhibitory concentrations ($IC_{50}$) than fosfomycin, a wellknown inhibitor of MurA. These inhibitors appear to covalently modify the sulfhydryl group of the active site cysteine (C117), since the C117D mutant Hi MurA was not inhibited by these compounds and excess dithiothreitol abolished their inhibitory activities. The increased mass value of Hi MurA after treatment with the identified inhibitor further confirmed that the active-site cysteine residue of Hi MurA is covalently modified by the inhibitor.

• KSBB Journal
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• v.25 no.6
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• pp.533-538
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• 2010

We investigated the effect of inhibitory compounds derived lignocellulosic hydrolysates on cell growth, sugar consumption and ethanol productivity, and also we intended to identify the potential for ethanol production based on lignocellulosic hydrolysates. Cell growth and ethanol production in the presence of acetate were initiated after 12 hr. Furans showed a longer lag time and phenolics showed a significant effect on strain and ethanol production in comparison to other model compounds. In the case of lignocellulosic hydrolysates, the acetate strongly affected cell growth and ethanol production.

• Archives of Pharmacal Research
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• v.29 no.11
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• pp.1006-1017
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• 2006

A series of 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one, 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione and 2, 2'-dithiobis 3-(substituted-benylidene)-1, 3-dihydro-indole derivatives was investigated as inhibitor of $p60^{c-Src}$tyrosine kinase by performing receptor docking studies and inhibitory activity toward tyrosine phosphorylation. Some compounds were shown to be docked at the site, where the selective inhibitor PP1 [1-tert-Butyl-3-p-tolyl-1H-pyrazolo[3,4-d]pyrimidine-4-yl-amine] was embedded at the enzyme active site. Evaluation of all compounds for the interactions with the parameters of lowest binding energy levels, capability of hydrogen bond formations and superimposibility on enzyme active site by docking studies, it can be assumed that 3-(substituted-benzylidene)-1, 3-dihydro-indolin-2-one and thione derivatives have better interaction with enzyme active site then 2, 2'-dithiobis 3-(substituted-benzylidene)-1, 3-dihydro indole derivatives. The test results for the inhibitory activity against tyrosine kinase by Elisa method revealed that 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione derivatives have more activity then 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one derivatives.

• Archives of Pharmacal Research
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• v.26 no.6
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• pp.463-465
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• 2003

Four protostane-type triterpenes, alisol B 23-acetate (1a), alisol C 23-acetate (2a), alisol B(3a), and alisol A 24-acetate (4a), were isolated from the rhizome of Alismatis plantago-aquatica L. var. orientale Samuelson (Alismataceae) and eleven protostane derivatives (compounds 1-11) were obtained by selective modification from alisol B 23-acetate (1a). These compounds were investigated for their anti-complement activity against the classical pathway of the complement system. Alisol B (3a) and alisol A 24-acetate (4a) exhibited anti-complement activity with $IC_{50} values of 150 and 130 \mu$ M. Among the synthetic derivatives, the tetrahydroxylated protostane triterpene (9) showed moderate inhibitory activity with $IC_{50} value of 97.1 \mu$ M. Introduction of an aldehyde group at C-23 (10; $IC_{50} value, 47.7 \mu$ M) showed the most potent inhibitory effect on the complement system in vitro.

• Journal of Ecology and Environment
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• v.29 no.4
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• pp.381-387
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• 2006

We analyzed the total yields and composition of essential oils in leaf extracts of Nepeta cataria by Gas Chromatography Mass Spectrometry (GC-MS). Thirty-six compounds representing 97.0% of total oil were detected. The major constituents of essential oils in Nepeta cataria were nepetalactone (90.9%), unidentified compound (Retention time 17.35; 1.82%), 1,8-cineol (1.49%), ${\beta}-caryophyllene$ (1.12%), and ${\beta}-pinene$ (1.078%). The volatile compounds in leaf extracts of N. cataria concentrated to nepetalactone ($88.83{\sim}93.33%$) remarkably. In the essential oil of N. cataria cis,trans-nepetalactone ($30.2{\sim}37.8%$) and cis,cis-nepetalactone ($31.5{\sim}37.0%$) were found as the main constituents. The effects of essential oil of N. cataria on the growth of six microorganisms (Bacillus cereus, B. subtilis, B. amyloliquefaciens, Escherichia coli, Staphylococcus aureus subsp. aureus, and Pseudomonas aeruginosa) were investigated. The essential oil of N. cataria had strong inhibitory effect on the growth of three fungal species (Bacillus cereus, B. subtilis, and B. amyloliquefaciens). The essential oil from N. cataria was found to have a low antimicrobial activity against Staphylococcus aureus subsp. aureus, while no activity were found against Escherichia coli and Pseudomonas aeruginosa. Results indicate the significant antimicrobial effect, which may be depended on the yield of nepetalactone.

• Archives of Pharmacal Research
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• v.29 no.7
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• pp.541-547
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• 2006

Four alkaloids (1-4), three quinolone alkaloids (5-7), and three flavanoid glucosides (8-10) were isolated from the fruits of Evodia officinalis Dode, and their structures were determined from chemical and spectral data. Compounds, 3, 8, 9 and 10 were isolated from this plant for the first time. Of these compounds, 1-3 and 5-7 exhibited moderate cytotoxicities against cultured human colon carcinoma (HT-29), human breast carcinoma (MCF-7), and human hepatoblastoma (HepG-2). Compound 8 showed strong inhibitory effects on DNA topoisomerases I and II (70 and 96% inhibition at a concentration of $20\;{\mu}M$, respectively).

• Journal of Integrative Natural Science
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• v.7 no.1
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• pp.45-49
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• 2014

The (c-Jun N-terminal kinase 3) JNK3 is a potential therapeutic target for various neurological disorders. Here, a three dimensional quantitative structure-activity relationship (3D-QSAR) study on phenoxypyridine as JNK3 inhibitors was performed to rationalize the structural requirements responsible for the inhibitory activity of these compounds. The comparative molecular field analysis (CoMFA) using different partial atomic charges, was employed to understand the structural factors affecting JNK3 inhibitory potency. The Gasteiger-Marsili yielded a CoMFA model with cross-validated correlation coefficient ($q^2$) of 0.54 and non-cross-validated correlation coefficient ($r^2$) of 0.93 with five components. Furthermore, contour maps suggested that bulky substitution with oxygen atom in $R^3$ position could enhance the activity considerably. The work suggests that further chemical modifications of the compounds could lead to enhanced activity and could assist in the design of novel JNK3 inhibitors.