• Title/Summary/Keyword: Compound Ⅲ

Search Result 11,918, Processing Time 0.044 seconds

Synthesis and Evaluation of Antitumor Activity of 2- and 6-[(1,3- Benzothiazol-2-yl)aminomethyl]-5,8-dimethoxy-1,4-naphthoquinone Derivatives

  • Chung, Yong-Seog;Shin, Young-Kook;Zhan, Chang-Guo;Lee, Sung-Duck;Cho, Hoon
    • Archives of Pharmacal Research
    • /
    • v.27 no.9
    • /
    • pp.893-900
    • /
    • 2004
  • 2- or 6-Substituted BZT-N derivatives were synthesized, and their cytotoxic activity against can-cer L1210 and SNU-1 cells was examined. The antitumor action was also assessed in mice bearing S-180 cells in peritoneal cavity. In a comparison, it was found that 6-substituted BZT-N derivatives exhibited higher potencies in both bioactivities than 2-substituted BZT-N derivatives against L1210 cells in in vitro and S-180 in vitro tests exception of compound 36. Interestingly, it was observed that 2-substituted compound 36, which has methyl group at RI position, exhib-ited a better antitumor activity than 6-substituted compounds against L1210 and SNU-1 in vitro. The EDso value of 2-substituted compound 36 against L1210 was found to be comparable to the EDso value of adriamycin and was even better against the solid cancer cell line SNU-1. It was also observed that 2-substituted compound 36 showed better antitumor activity in mice bearing S-180 cells in the peritoneal cavity. The T/C (%) value of 2-substituted compound 36 was simi-lar to that of adriamycin. Quantitative structure-activity relationship (QSAR) tests reveal that the experimental E $D_{50}$ values against SNU-1 closely correlate with both the calculated HOMO ener-gies ( $E_{HOMO}$) and the measured H-NMR chemical shift of 3-H ($\delta$$_{H}$). The results suggests that a compound having higher $E_{HOMO}$ and $\delta$$_{H}$ values usually should have a lower E $D_{50}$ (SNU-1) value.lue.lue.lue.

The Effect of N-Substituted Alkyl Groups on the Anticonvulsant Activities of N-Cbz-${\alpha}$-amino-N-alkylsuccinimides

  • Lee, Jae-Won;Son, Ki-Chun;Jung, Kyung-Im;Choi, Jong-Won;Park, Min-Soo
    • Archives of Pharmacal Research
    • /
    • v.20 no.1
    • /
    • pp.53-57
    • /
    • 1997
  • For the purpose of defining the effects of the N-substituted alkyl groups on the anticonvulsant activities of N-Cbz-.alpha.-aminosuccinimides, various (R)- and (S)-N-alkyl substituted N-Cbz-.alpha.-aminosuccinimides (1 and 2) were prepared from the corresponding (R)- and (S)-N-Cbz-aspartic acid by using known reaction and were evaluated the anticonvulsant activies in the MES and PTZ tests, including their neurotoxicities. The most active compound in the MES test was (R)N-Cbz-.alpha.-amino-N-methylsuccinimide (1b) $(ED_{50}=52.5 mg/kg, Pl=3.2)$. And in case of the PTZ test, (R)-N-Cbz-.alpha.-amino-N-ethylsuccinimide (1c) was the most active compound $(ED_{50}/=32.5mg/kg, Pl=3.1)$. The order of anticonvulsant activities of these compounds against the MES test, as judged from the ED_50values for the R series (1), was N-methyl > N-isobutyl > non-substituted > N-ethyl, N-allyl > N-benzyl compound; for the S series (2) N-methyl > N-altyl > non-substituted > N-isobutyl > N-ethyl > N-benzyl compound. The anticonvulsant activities in the PTZ tests of these compounds exhibited somewhat different pattern ; for the R series (1) Nethyl > N-methyl > N-isobutyl> non-substituted > N-allyl > N-benzyl compound in order of decreasing activity; for S series (2) N-ethyl > N-allyl, non-substituted > N-isobutyl > N-methyl > N-benzyl compound in order of decreasing activity.

  • PDF

Photo-Induced Chemical Vapor Deposition of $SiO_2$ Thin Film by Direct Excitation Process (직접 광여기 Photo-CVD에 의한 이산화실리콘 박막의 증착 특성)

  • Kim, Youn-Tae;Kim, Chi-Hoon;Jung, Ki-Ro;Kang, Bong-Ku;Kim, Bo-Woo;Ma, Dong-Sung
    • Journal of the Korean Institute of Telematics and Electronics
    • /
    • v.26 no.7
    • /
    • pp.73-82
    • /
    • 1989
  • We developed a photo-CVD equipment for the deposition of silicon based insulating materials. Silicon dioxide thin films were deposited at various process conditions especially low temperature range $50-250^{\circ}C$. Low pressure mercury lamp was used in the direct excitation of $SiH_4/N_2O$ mixture gas without mercury sensitization. AES and ESCA analysis showed that oxygen to silicon atomic ratio and binding state of Si-O bond was nearly 2.0 and $SiO_2$ type, respectively. The refractive indices were measured to be 1.39-1.44, indicating that films were in relatively low density.

  • PDF

Effects of Dietary Supplementation with a Compound Composed of Caffeine, Capsaicin, Sesamine, L-Carnitine, Banaba and Lotus on Human Autonomic Nervous System Activity and Lipid Oxidation

  • Kang, Sung-Hwun;Shin, Ki-Ok
    • Preventive Nutrition and Food Science
    • /
    • v.14 no.3
    • /
    • pp.173-178
    • /
    • 2009
  • This study was conducted to determine if supplementation with a compound composed of caffeine (50 mg), capsaicin (75 mg), sesamine (30 mg), L-carnitine (300 mg), banaba (50 mg) and lotus (10 mg) enhanced human autonomic nervous activities (ANS) associated with thermogenic sympathetic activity and fat utilization. Ten healthy college males (21.2$\pm$1.0 yr) volunteered for this experiment. Autonomic nervous activities associated with energy metabolism were examined at 30 min intervals for a total of 120-min while at rest and every 5-min during exercise at 50% of the ventilation threshold before and after intake of the compound or placebo with 100 ml of water for 10 days. In addition, heart rate variability power spectral analysis was used to assess human autonomic nervous activities. The results indicated that there were no significant differences in heart rate during rest and exercise among trials. Furthermore, the autonomic nervous activity tended to increase after 10-days of consumption of the test compounds during the experimental period, but the differences did not reach statistical significance. However, before and after the compound test trial there was a significantly higher respiratory gas exchange ratio (rest 0: 0.83$\pm$0.01 vs. rest 3: 0.89$\pm$0.02, p<0.05), carbohydrate oxidation (CHO) rate (rest 0: 44.57$\pm$5.83 vs. rest 2: 63.86$\pm$5.91%, p<0.05) and a lower fat oxidation rate (rest 0: 55.43$\pm$5.83 vs. rest 2: 36.14$\pm$5.91%, p<0.05. In conclusion, the results of the present study suggested that the compound composed of caffeine, capsaicin, sesamine, L-carnitine, banaba and lotus components that was evaluated in this study did not induce a significant increase in human autonomic nervous activities or lipolysis, even though the individual components have been reported to induce increased fat oxidation.

A Study on Interior Design of Compound Bookstore Based on the Concept of Service Design (서비스 디자인 개념에 기초한 복합형 서점 실내 디자인 연구)

  • Pan, Ying-Ying;Kim, Myung-Soo
    • Journal of the Korea Convergence Society
    • /
    • v.11 no.1
    • /
    • pp.97-108
    • /
    • 2020
  • Nowadays, '1+N' is the operation model of compound bookstores. This study firstly investigated the general information and needs of customers and analyzed 4 basic behaviors of customers in 10 functional space of bookstore. Secondly, a preliminary analysis framework of interior design of compound bookstore was established, by applying 3 research tools of service design to 3 design elements of interior design. Thirdly, the case was analyzed in the preliminary analysis framework to find out the detailed process of the interaction between the customer and the bookstore, the touchpoint and the interior design project, to find out the blind spots in design, and put forward the solutions. Finally, after being refined, a compound bookstore interior design model based on the concept of service design was established. This model can be used to test the design content and service quality of the interior functional area of the compound bookstore, and to find out the design blank points.

Antipruritic Effects of Ethanol Extracts from Perillae Japonicae Semen leaves and Chaenomelis Fructus (임자잎과 모과 에탄올 추출물의 피부 가려움증 억제 효과)

  • Kim, Hyeon-Soo;Jeon, In-Hwa;Mok, Ji-Ye;Kang, Hyun-Ju;Jang, Seon-Il
    • Journal of Physiology & Pathology in Korean Medicine
    • /
    • v.26 no.3
    • /
    • pp.314-319
    • /
    • 2012
  • Itching is one of the major diagnostic criteria of atopic dermatitis (AD) and one of its most troublesome symptoms that provokes the desire to scratch. Effective control of itching is believed to be one of the basic approaches in controlling AD. The purpose of this study was undertaken to investigate the antipruritic effect of ethanol extracts from Perillae Japonicae Semen leaves (PJSL) and Chaenomelis Fructus (CF) on the scratching behavior induced by pruritogen such as compound 48/80 or substance P in hairless mice. PJSL or CF treatment inhibited histamine release in HMC-1 stimulated compound 48/80 or substance P in a dose-dependant manner. In particularly, co-treatment PJSL ($50{\mu}g/mL$) plus CF ($100{\mu}g/mL$) significantly inhibited histamine release in HMC-1 stimulated compound 48/80 or substance P. PJSL, CF or PJSL plus CF was administered orally for 2 h and then compound 48/80 ($50{\mu}g/site$) or substance P ($100{\mu}g/site$) was injected into rostral back, and scratching of the injected site by the hind paw was counted for 1 h. PJSL or CF administration reduced the scratching behavior induced by compound 48/80 as well as substance P in a dose-dependent manner. Furthermore, co-administration of PJSL and CF markedly suppressed the scratching behavior induced by compound 48/80 as well as substance P. These suppressive effects were synergistically increased by their combination. From the preliminary observations, we considered that ethanol extracts from PJSL and CF could be an effective natural materials for itching treatment.

Effective Thematic Words Extraction from a Book using Compound Noun Phrase Synthesis Method

  • Ahn, Hee-Jeong;Kim, Kee-Won;Kim, Seung-Hoon
    • Journal of the Korea Society of Computer and Information
    • /
    • v.22 no.3
    • /
    • pp.107-113
    • /
    • 2017
  • Most of online bookstores are providing a user with the bibliographic book information rather than the concrete information such as thematic words and atmosphere. Especially, thematic words help a user to understand books and cast a wide net. In this paper, we propose an efficient extraction method of thematic words from book text by applying the compound noun and noun phrase synthetic method. The compound nouns represent the characteristics of a book in more detail than single nouns. The proposed method extracts the thematic word from book text by recognizing two types of noun phrases, such as a single noun and a compound noun combined with single nouns. The recognized single nouns, compound nouns, and noun phrases are calculated through TF-IDF weights and extracted as main words. In addition, this paper suggests a method to calculate the frequency of subject, object, and other roles separately, not just the sum of the frequencies of all nouns in the TF-IDF calculation method. Experiments is carried out in the field of economic management, and thematic word extraction verification is conducted through survey and book search. Thus, 9 out of the 10 experimental results used in this study indicate that the thematic word extracted by the proposed method is more effective in understanding the content. Also, it is confirmed that the thematic word extracted by the proposed method has a better book search result.

Study on the Wear Resistant Characteristics of Medium Carbon Alloy Steel Plasma-Nitrided (플라즈마 질화처리된 중탄소합금강의 내마모특성에 관한 연구)

  • Cho, H.S.;Roh, Y.S.;Shin, H.K.;Lee, S.Y.
    • Journal of the Korean Society for Heat Treatment
    • /
    • v.5 no.4
    • /
    • pp.215-223
    • /
    • 1992
  • This study has been performed to investigate into some effects of temperature, gas mixing ratio and time on the optical microstructure, hardness and wear characteristics of medium carbon alloy steel treated by plasma nitriding. The results obtained from the experiment are summarized as follows: (1) Optical micrographs of AISI 4140 steel plasma-nitrided by the double stage technique have revealed that the nitrided layer is composed of the compound layer and the diffusion layer. The variation in temperature at the first stage gives effects, on the formation of compound layer and the growth rate is shown to be relatively fast at $460^{\circ}C$. (2) The thickness of compound layer has been found to increase with increasing nitrogen percentage in the gas mixture and the holding time. It is therefore recommended that a shorter holding time and a lower nitrogen percentage are more effective to produce a tougher compound layer and a diffusion layer only. (3) X-ray diffraction analysis for AISI 4140 steel has shown that the compound layer consist of ${\gamma}^{\prime}-Fe_4N$ and ${\alpha}-Fe$ and that tough compound layer diffustion layer only can be obtained by the double stage plasmanitriding process. (4) There is also a tendency that the total hardened layer depth increases with increasing temperature, time and nitrogen percentage in the first stage during the double stage plasma nitriding. (5) The wear resistance of plasma nitrided specimens has been found thobe considerably increased compared to the untreated specimens and the amount of increment has appeared to increase further with increasing nitriding temperature, holding time and notrogen percentage of gas mixture in the first stage treatment.

  • PDF

A Study on the Wear Characteristics of Compound Layers Formed during Gaseous Nitrocarburizing in Medium Carbon Boron Steels (중탄소 Boron강의 가스침질탄화처리에 의해 형성된 화합물층의 마모특성에 관한 연구)

  • Park, K.W.;Oh, D.W.;Cho, H.S.;Lee, H.W.;Lee, J.B.;Lee, S.Y.
    • Journal of the Korean Society for Heat Treatment
    • /
    • v.12 no.2
    • /
    • pp.136-144
    • /
    • 1999
  • The study on the wear characteristics of compound layers formed during gaseous nitrocarburising in the medium carbon boron steels and the plain carbon steel has been carried out by using a pin-on-disc type wear test machine under the oil lubricating condition at room temperature and by varying applied loads, sliding speeds and wear distances. Values of friction coefficient measured at the sliding speed of 0.4m/sec under the oil lubricating condition have been shown to decrease considerably with increasing applied load and become gradually a constant value as load is increased to a higher value, showing that the transition load for friction coefficient appears at an applied load of 247.2N. The length and volume wear rates of compound layer have been revealed to relatively constantly increase, also showing that the wear life per unit thickness of compound layer turns out to be superior as porous layer has a denser and thinner appearance. As the sliding speed increases during wear test performed by varying sliding speed at a load of 63.2N under the oil lubricating condition for medium carbon boron steel nitrocarburised in gas atmosphere, the wear rate has been found to increase, the friction coefficient to decrease and the wear life per unit thickness of compound layer to decrease considerably.

  • PDF

Synthesis and $^{18}F$ Labelling of Organic Ammonium Salts to New Cardiac Flow Tracer for PET and Their Biodistribution (양전자단층촬영에 이용 가능한 새로운 심근 혈류 추적자 개발; F-18이 표지된 유기암모늄염의 합성과 체내분포에 관한 연구)

  • Yu, Kook-Hyun
    • The Korean Journal of Nuclear Medicine
    • /
    • v.28 no.3
    • /
    • pp.331-337
    • /
    • 1994
  • In order to develop a $^{18}F$-labelled myocardial perfusion agent(flow tracer) for PET, $^{18}F$-labelled organic ammonium cations were synthesized and evaluated in relation to their biodistribution. Five quaternary organic ammonium compounds were labelled with $^{18}F$ in a side chain with moderate to good yields by direct introduction of $^{18}F$-fluoride. Radiochemical yields have been achieved in 30-40min by the precursors (tosylates) in dimethylsulfoxide 15-60% (decay corrected). The reaction was found to be autocatalyzed. A remote controlled procedure was developed in these synthesis. $^{18}F$-Labelling and HPLC-purification of com-pounds needed about 60 min(Yield; 7-20%). Up to now the two compounds N-4-[$^{18}F$]fluorobutyl-pyridinium cation(1) and N, N dibenzyl-4(2-[$^{18}F$]fluoroethyl)piperidinium cation(2) were investigated in relation to their biodistribution in mice. Compound 1 showed at 1 min post injection the high uptake of 19.22% ID/g organ in the myocardium but a following fast decline to 1.12% ID/g organ after 40min. Uptake of compound 2 was after 1min in the heart 5.90% ID/g organ but after 40min at the relative high value of 4.33% ID/g organ. Heart:blood ratio for compound(1) at 1 min was 8.3, at 40 min 2.6 for compound II 2.0(1min) and 15.0(40 min). As data of compound 2 showed greater heart uptake, slower myocardial release, and higher heart: blood ratios, compound 2 is a good candidate for further evaluation.

  • PDF