• Title/Summary/Keyword: $4{alpha}$

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Butyrylcholinesterase Inhibitory Guaianolides from Amberboa ramosa

  • Khan Sher Bahadar;Haq Azhar-ul;Perveen Shagufta;Afza Nighat;Malik Abdul;Nawaz Sarfraz Ahmad;Shah Muhammad Raza;Choudhary Muhammad lqbal
    • Archives of Pharmacal Research
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    • v.28 no.2
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    • pp.172-176
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    • 2005
  • Phytochemical investigation of the whole plant of Amberboa ramosa led to the isolation of six sesquiterpene lactones which could be identified as $8{\alpha}$-hydroxy-$11{\beta}$-methyl-$1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H,\;11{\alpha}H-guai-10(14)$, 4(15)-dien-6, 12-olide(2), $3{\beta},\;8{\alpha}-dihydroxy-11{\alpha}-methyl-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H,\;11{\beta}H-guai-10(14)$, 4(15)-dien-6, 12-olide (2), $3{\beta},\;4{\alpha},\;8{\alpha}-trihydroxy-4{\beta}(hydroxymethyl)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$, 11(13)-dien-6, 12-olide (3), $3{\beta},\;4{\alpha},\;8{\alpha}-trihydroxy-4{\beta}-(chloromethyl)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$, 11(13)-dien-6, 12-olide(4), $3{\beta},\;4{\alpha},\;dihydroxy-4{\beta}-(hydroxymethyl)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$, 11(13)-dien-6, 12-olide(5), $3{\beta},\;4{\alpha}-dihydroxy-4{\beta}-(chloromethyl)-8{\alpha}-(4-hydroxymethacrylate)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$, 11(13)-dien-6, 12-olide (6) by spectroscopic methods. All of them showed inhibitory potential against butyrylcholinesterase.

Synthesis of -4,9-Dione Derivatives (벤조-[f]-인돌-4, 9-디온 유도체의 합성)

  • Lee, Ji-Young;Suh, Myung-Eun
    • YAKHAK HOEJI
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    • v.34 no.1
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    • pp.15-21
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    • 1990
  • -4,9-dione derivatives were prepared from $2-chloro-3-({\alpha}-accetyl-{\alpha}-ethoxycarbonyl-methyl)-1,4-naphthoquinone$ and 2-chloro-3-N-phenylamino-1,4-naphthoquinone. $2-Chloro-3-({\alpha}-acetyl-{\alpha}-ethoxycarbonyl-methyl)-1,4-naphthoquinone$ was reacted with amines to give $2-amino-3-({\alpha}-acetyl-{\alpha}-ethoxycarbonyl-methyl)-1,4-naphthoquinone$ derivatives. Subsequent treatment of $2-amino-3-({\alpha}-acetyl-{\alpha}-ethoxycarbonyl-methyl)-1,4-naphthoquinone$ with sodium ethoxide gave -4,9-dione derivatives. When 2-chloro-3-N-phenylamino-1,4-naphthoquinone reacted with sodium ${\alpha}-cyano$ ethyl acetate, 2-amino-3-ethoxycarbonyl-N-phenyl--4,9-dione was obtained. However, with sodium diethyl malonate, not -4,9-dione but 2-chloro-3-bis-(methoxycarbonyl)-methyl-2H-3-N-phenylamino-1,4-naphthoquinone was obtained.

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$\alpha$ to $\beta$ Phase Transformation of $\alpha$-Si3N4 Whisker ($\alpha$-질화규소 Whisker의 $\alpha$/$\beta$ 상변태)

  • 박지연;김종희
    • Journal of the Korean Ceramic Society
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    • v.25 no.5
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    • pp.502-508
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    • 1988
  • The $\alpha$ to $\beta$ phase transformation of $\alpha$-Si3N4 whisker and related microstructural changes have been investigated. When only $\alpha$-Si3N4 whisker was heat treated in the range 1650~175$0^{\circ}C$, the $\alpha$ to $\beta$ phase transformation occured. In this case, it eas suggested that the oxygen content in $\alpha$-Si3N4 whisker affected the transformation behavior. Although $\alpha$-Si3N4 whisker with Si was heat treated under the same condition, however, the variation of $\beta$- fraction had a similar tendency with heat treating time. Therfore, it was considered that the oxygen content in $\alpha$-Si3N4 whisker affected the transformation behavior dominently rather than the content of added Si. The added $\beta$ phase did not affect the transformation behaviro of $\alpha$-Si3N4 whisker.

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Sesquiterpene Lactones of Artemisia sylvatica (그늘쑥의 Sesquiterpene Lactone 성분)

  • 권학철;최상진;이원빈;민용득;양민철
    • YAKHAK HOEJI
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    • v.45 no.2
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    • pp.147-152
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    • 2001
  • The phytochemical study of the aerial parts of Artemisia sylvatica (Asteraceae) led to the isolation of nine sesquiterpene lactones, l$\alpha$-hydroperoxy-rupicolin A acetate (1), rupicolin B acetate (2), rupicolin A acetate (3), l$\alpha$-hydroxy-4$\alpha$-hydroperoxy-bishopsolicepolide (4), 1$\alpha$-hydroperoxy-4$\beta$-hydroxy-8$\alpha$-acetoxy-guaia-2,9,11 (13)-triene-6$\alpha$,12-oxide (5), 1$\alpha$-hydroperoxy-4$\alpha$-hydroxybishopsolicepolide (6), l$\alpha$,4$\beta$-dihydroxy-8$\alpha$-acetoxy-guaia-2,9,11(13)-triene-6$\alpha$,12-olive (7), rupicolin A (8) and l$\alpha$,4$\alpha$-dihydroxy-bishopsolicepolide (9). Their structures were established by chemical and spectroscopic methods.

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Microbial $9{\alpha}$-Hydroxylase:Epoxidation of 9(11)-dehydro-$17{\alpha}$-methyl-testosterone

  • Kang, Hee-Kyoung;Lee, Sang-Sup
    • Archives of Pharmacal Research
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    • v.20 no.6
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    • pp.525-528
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    • 1997
  • Steroid $9{\alpha}$.-hydroxylase is a key enzyme system in steroid nucleus degradation in company with ${\Delta}$-dehydrogenase. To examine $9{\alpha}$-hydroxylase activity during microbial transformation of steroids, 9(11)-dehydro-$17{\alpha}$-methyl-testosterone was adopted as a stable substrate for preventing the rupture of steroid nucleus. Using Nocardia restrictus ATCC 14887 capable of introducing a $9{\alpha}$-hydroxyl group into steroids, $9{\alpha}$,$11{\alpha}$-oxido-$17{\beta}$-hydroxy-$17{\alpha}$-methyl-4-androstene-3-one and $9{\alpha}$-hydroxyl group into steroids,$9{\alpha}$,$11{\alpha}$-oxido-$17{\beta}$-hydroxy-$17{\alpha}$-methyl-1,4-androstadiene-3- one were obtained. These microbiologically transformed products could be used as reference compounds in the enzyme assay.

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Characterization of Extracellular \alpha-galactosidase Produced by Streptomyces sp. YB-4. (균체외 \alpha-galactosidase를 생산하는 Streptomyces sp. YB-4의 분리 및 효소 특성)

  • 김소영;조기행;김창진;박동진;윤기홍
    • Microbiology and Biotechnology Letters
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    • v.30 no.4
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    • pp.332-338
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    • 2002
  • A strain YB-4 producing the extracellular $\alpha$-galactosidase was isolated from soil, and has been identified as Streptomyces sp. on the basis of its cultural, morphological and physiological properties. The partially purified $\alpha$-galactosidase was most active on paranitrophenyl-$\alpha$-D-galactopyranoside at pH 6.0 and 6$0^{\circ}C$. The enzyme retained 90% of its maximum activity between pH 4.0 and pH 10.0 after pre-incubation for 1 h. The enzyme was able to hydrolyze oligomeric substrates such as melibiose, raffinose and stachyose to liberate galactose residue, indicating that the $\alpha$-galactosidase of Steptomyces sp. YB-4 hydrolyzed $\alpha$-1,6 linkage.

New inhibitors of the NF-kB activation and NO production from Artemisia sylvatica

  • Jin, Huizi;Lee, Jeong-Hyung;Lee, Dong-Ho;Kim, Young-Ho;Lee, Jung-Joon
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.67.1-67.1
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    • 2003
  • Three new guaianolide type of sesquiterpene lactones, 8${\alpha}$-angeloyloxy-1${\alpha}$-hydroxy-3${\alpha}$,4${\alpha}$-epoxy-5${\alpha}$, 7${\alpha}$H-10(14), 11(13)-guaiadien-12,6${\alpha}$-olide (1), 8${\alpha}$-methylbutyryloxy-1${\alpha}$-hydroxy-3${\alpha}$, 4${\alpha}$-epoxy-5${\alpha}$, 7${\alpha}$H-10(14),11(13)-guaiadien-12,6${\alpha}$-olide (2), and 8${\alpha}$-isovaleryloxy-1${\alpha}$-hydroxy-3${\alpha}$, 4${\alpha}$-epoxy-5${\alpha}$, 7${\alpha}$H-10(14),11 (13)- guaiadien-12,6${\alpha}$-olide (3), together with six known sesquiterpenes, artemisolide (4), 3-methoxytanapartholide (5), deacetyllaurenobiolide (6), moxartenolide (7), arteminolide B (8), and arteminolide D (9) were isolated by bioassay-guided fractionation using the NF-kB mediated reporter gene assay system. (omitted)

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Synthesis of Indoprofen (Indoprofen의 합성)

  • 최홍대;강병원;마정주;윤호상
    • YAKHAK HOEJI
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    • v.35 no.4
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    • pp.314-318
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    • 1991
  • A convenient method for the synthesis of indoprofen, which is a potent antiinflammatory agent, w described. Ethyl $\alpha$-(4-aminophenyl)propionate was prepared by nitration of ethyl $\alpha$-phenylpropionate, followed by reduction. Ethyl $\alpha$-[4-(1, 3-dioxo-2-iso-indolinyl)phenyl]propionate was obtained from condensation reaction of phthatic anhydride and ethyl $\alpha$-(4-aminophenyl)propionate. Indoprofen was prepared by reduction of ethyl $\alpha$-[3-(1, 3-dioxo-2-iso-indolinyl)phenyl]propionate with zinc dust-acetic acid, followed by hydrolysis of the resultant ethyl $\alpha$-[4-(1-oxo-2-iso-indolinyl)pheriyl]propionate.

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Stereoselective synthesis of novel 4′$\alpha$-C-methyl branched novel carbocyclic nucleosides

  • Kim, Ji-Hee;Ko, Ok-Hyun;Hong, Joon-Hee
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.345.2-345.2
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    • 2002
  • Recently. 4'${\alpha}$-C homologated furanose nucleosides. especially alkyl branches. are molecules of considerable current interest. One of reasons for this prominence arises from the notable biological activities as antiviral and antitumor agents. as shown in 4'${\alpha}$-C-methyl-2-deoxythymidine (EC$_{50}$ = 7.2$\mu$M against HIV in MT-4 cell), 4'${\alpha}$-C-fluoromethyl-2-deoxycytidine. 4'${\alpha}$-C-hydroxymethylthymidine and 4'${\alpha}$- -C-azidomethyl-thymidine. (omitted)omitted)

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