• Title/Summary/Keyword: novel compound

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The Disperse Dyeing of Polyester/Cotton Blend Using a Hetero-bifunctional Bridge Compound (I) (이반응형 브리지 화합물을 이용한 폴리에스테르/면 복합소재의 단일분산염료염색 (I))

  • Kim Tae-Kyeong;Yoon Seok-Han;Kim Mi-Kyung
    • Textile Coloration and Finishing
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    • v.18 no.3 s.88
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    • pp.1-9
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    • 2006
  • In order to dye polyester/cotton blend fabric by one-bath dyeing process with single disperse dye, a novel hetero-bifunctional bridge compound(DBDCBS) was synthesized and utilized. The DBDCBS was designed to contain two different reactive groups such as ${\alpha},{\beta}$-dibromopropionylamido and dichloro-s-triazinyl groups. The ${\alpha},{\beta}$-dibromopropionylamido group shows considerable reactivity towards amines or amino groups at acidic condition and high temperature. In contrast, the dichloro-s-triazinyl group has reactivity towards hydroxyl groups at alkaline condition and room temperature. In order to examine whether as a bridge the compound could combine dyes containing amino groups with cellulosic substrates, disperse dyes containing amino group were tried to dye the cotton fibers pretreated with the DBDCBS compound. By the results, polyester/cotton blends were dyed by one-bath dyeing process with single disperse dye,1,4-diaminoanthraquinone.

Identification of a Novel Small Molecule Inhibitor Against SARS Coronavirus Helicase

  • Cho, Jin-Beom;Lee, Jin-Moo;Ahn, Hee-Chul;Jeong, Yong-Joo
    • Journal of Microbiology and Biotechnology
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    • v.25 no.12
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    • pp.2007-2010
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    • 2015
  • A new chemical inhibitor against severe acute respiratory syndrome (SARS) coronavirus helicase, 7-ethyl-8-mercapto-3-methyl-3,7-dihydro-1H-purine-2,6-dione, was identified. We investigated the inhibitory effect of the compound by conducting colorimetry-based ATP hydrolysis assay and fluorescence resonance energy transfer-based double-stranded DNA unwinding assay. The compound suppressed both ATP hydrolysis and double-stranded DNA unwinding activities of helicase with IC50 values of 8.66 ± 0.26 μM and 41.6 ± 2.3 μM, respectively. Moreover, we observed that the compound did not show cytotoxicity up to 80 μM concentration. Our results suggest that the compound might serve as a SARS coronavirus inhibitor.

Synthesis and de-pigmentation effect of phenolic glucoconjugates

  • Kim, Ki-Ho;Kim, Ki-Soo;Lee, Jae-Soeb;Ko, Kang-Il;Lee, Soo-Hee
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.27 no.1
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    • pp.99-109
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    • 2001
  • Novel glucoconjugates phenolic moiety, 3-(methoxycarbonyl)-4-(hydroxyphenyl)-$\beta$-D-glucopyranoside(4), 3-(methoxyacetyl)-4-(hydroxyphenyl)-$\beta$-D-glucopyranoside(7), 4-(hydroxyphenyl)-$\beta$-D-ribofuranoside(11), were synthesized. In order to investigate their depigmentation effect, inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in B16 melanoma cell were evaluated in vitro. Compound 11 showed 92.0$\mu\textrm{g}$/㎖ of tyrosinase inhibitory activity whereas compound 4 and 7 showed very low activity not less than 300$\mu\textrm{g}$/㎖. Inhibitory activities of melanin synthesis in B16 melanoma cell of compound 4, 7, and 11 were 8.7, 15.1, and 36.0%, respectively, at the concentration of 100$\mu\textrm{g}$/㎖. Inhibitory activity of compound 11 was much higher than that of arbutin at the same concentration.

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Gut microbiota-mediated pharmacokinetics of ginseng saponins

  • Kim, Dong-Hyun
    • Journal of Ginseng Research
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    • v.42 no.3
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    • pp.255-263
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    • 2018
  • Orally administered ginsengs come in contact with the gut microbiota, and their hydrophilic constituents, such as ginsenosides, are metabolized to hydrophobic compounds by gastric juice and gut microbiota: protopanxadiol-type ginsenosides are mainly transformed into compound K and ginsenoside Rh2; protopanaxatriol-type ginsenosides to ginsenoside Rh1 and protopanaxatriol, and ocotillol-type ginsenosides to ocotillol. Although this metabolizing activity varies between individuals, the metabolism of ginsenosides to compound K by gut microbiota in individuals treated with ginseng is proportional to the area under the blood concentration curve for compound K in their blood samples. These metabolites such as compound K exhibit potent pharmacological effects, such as antitumor, anti-inflammatory, antidiabetic, antiallergic, and neuroprotective effects compared with the parent ginsenosides, such as Rb1, Rb2, and Re. Therefore, to monitor the potent pharmacological effects of ginseng, a novel probiotic fermentation technology has been developed to produce absorbable and bioactive metabolites. Based on these findings, it is concluded that gut microbiota play an important role in the pharmacological action of orally administered ginseng, and probiotics that can replace gut microbiota can be used in the development of beneficial and bioactive ginsengs.

Synthesis of Novel Kojic Acid Derivatives and Their Tyrosinase Inhibitory Activities (새로운 코직산 유도체의 합성과 티로시나제 저해활성)

  • 김지연;임세진
    • YAKHAK HOEJI
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    • v.43 no.1
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    • pp.28-32
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    • 1999
  • Four derivatives of kojic acid were synthesized and their inhibitory activities against tyrosinase were evaluated. The C-2 hydroxymethyl and C-7 hydroxyl of kojic acid were replaced by carboxylate and amine, respectively. These derivatives were coupled to L-phenylalanine, producing two amide compounds. The carboxylate derivative (3), its amide compound (5), and the amine derivative (7) were weak inhibitors. The amide compound (9) where amine derivative (7) coupled to L-phenylalanine showed strong inhibitory activity ($IC_{50}=24.6{\;}{\mu}M$) comparable to kojic acid.

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Identification of Novel Saringosteryl Glucoside in Phaseolus vulgaris Seed (강낭콩 미숙종자내 신규 Saringosteryl Glucoside의 동정)

  • 김성기
    • Journal of Plant Biology
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    • v.37 no.4
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    • pp.441-444
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    • 1994
  • From immature seed of Phaseolus vulgaris L., a novel phytosteryl glucoside was isolated. Strong ion peaks at m/z 613 $[M+Na}^{+},\;696\;[M+Matrix]^{+}$ in positive F AB- MS and at m/z 589 $[M-1]^{-}$ in negative F AB- MS indicated the molecular weight of the compound is 590. Four hundred MHz $^IH-NMR$ analysis revealed that the compound canys a 24-hydroxy-24-vinyl-cholesterol (saringosterol) as an aglycone and a ${\beta}-D-glucopyranose$. Four hundred MHz $^IH-NMR$ analysis of the acetate derivate of the compound revealed that hydroxyls at C-1' in glucose moeity and at C-3 in aglycone have been condensed. Therefore, the phytosteryl glucoside was characterized to be $3-0-{\beta}-D-glucopyranosyl-24-hydroxy-24-vinyl-cholesterol$ (saringosteryl glucoside). This is the first demonstration for the presence of saringosterol in higher plants. Also this is the first identification of saringosteryl glucoside in natural materials.erials.

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Stereoselective Synthesis of a Novel Cyclohexene Version of Carbovir

  • Li, Hua;Hong, Joon-Hee
    • Bulletin of the Korean Chemical Society
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    • v.28 no.10
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    • pp.1645-1650
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    • 2007
  • This paper describes a racemic and stereoselective synthetic route for a novel cyclohexenyl carbocyclic adenine analogue. The required stereochemistry of the target compound was controlled using a stereoselective glycolate Claisen rearrangement followed by α-chelated carbonyl addition. The introduction of 6-chloropurine was achieved using Mitsunobu conditions, and further modifications of the corresponding heterocycle gave the target cyclohexenyl nucleoside.

A Novel Photonuclease; Bromofluoroacetophenone Analogs

  • Jeon, Raok
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2001.11a
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    • pp.81-81
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    • 2001
  • The photoinducible DNA cleaving activities of bromofluoroacetophenones as a novel photonuclease were investigated. The photolytic behavior and DNA cleaving acitivity of fluorine derivative were compared with those of non-fluorine substituted compound, 4'-bromoacetophenones. Although the DNA cleaving activities of fluorine analogs were similar with those of 4'-bromoacetophenones, ο-bromo-$\rho$-fluoro derivatives gave the better DNA cleaving activities than $\rho$-bromo-ο-fluoro derivatives did.

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Syntheses of Novel 10-Oxodaunomycinone Derivatives (새로운 10-옥소다우노마이시논 유도체의 합성)

  • 노영쇠;김선자;조인호;신홍식
    • YAKHAK HOEJI
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    • v.43 no.1
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    • pp.11-15
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    • 1999
  • A brief route for regiospecific synthesis of novel 10-Oxodaunomycinone Derivatives (10a, b) is described. Dimethoxy-l-tetralone 4 was converted to acetyl tetralone (5a, b) which was oxidized with oxygen to obtain cis-diol compound (8a, b). The construction of (10a, b) was completed by the condensation of phthaloyl dichloride 9 with cis-diol (8a, b)

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Metabolism of YH3945, a novel anticancer drug, in rats using 14C-labeled compound

  • Lee, Jae-Ick;Son, Jung-Hyun;Ahn, Byung-Nak;Lee, Bong-Yong;Kim, Dong-Hyun
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.130.1-130.1
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    • 2003
  • The metabolism of a novel anticancer agent 1-{3- [3-(4-Cyano -benzyl)-3H-imidazol-4-yl]-propyl }-3-(6-methoxy-pyridin-3-yl)-1-(2-trifluoromethyl-benzyl)-thiourea (YH3945) were investigated in the Sprague-Dawley rat after single oral and i.v. administration of [14C]-YH3945. Bile, feces, urine and plasma were collected and analyzed by an HPLC system equipped with multiple detectors. (omitted)

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