• Archives of Pharmacal Research
• /
• 제28권2호
• /
• pp.172-176
• /
• 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.

• 약학회지
• /
• 제37권1호
• /
• pp.49-53
• /
• 1993

Arylalkanoic acid derivatives are known as good non-steroidal antiinflamatory and antirheumatic agents. The new arylalkanoic acid derivatives were synthesized when 2-chloro-3-($\alpha$-cyano-$\alpha$-ethoxycarbonyl-methyl)-1, 4-naphthoquinone was reacted with some arylamines.

• 약학회지
• /
• 제34권1호
• /
• pp.15-21
• /
• 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.

• 한국세라믹학회지
• /
• 제25권5호
• /
• pp.502-508
• /
• 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.

• 약학회지
• /
• 제45권2호
• /
• pp.147-152
• /
• 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.

• Archives of Pharmacal Research
• /
• 제20권6호
• /
• pp.525-528
• /
• 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.

• 한국미생물·생명공학회지
• /
• 제30권4호
• /
• pp.332-338
• /
• 2002

토양으로부터 세포외로 $\alpha$-galactosidase를 분비 생산하는 방선균 YB-4가 분리되었으며, 분리균의 배양ㆍ형태ㆍ생리적 특성을 조사한 결과 Streptomyces 속 균주로 확인되었다. 분리균의 배양상등액으로부터 부분정제된 $\alpha$-galactosidase를 조효소액으로 사용하였을 때 para-nitrophenyl-$\alpha$-D-galacto-pyranoside는 pH 6.0과 6$0^{\circ}C$의 반응조건에서 가장 잘 분해되었으며, 조효소액을 pH 4.0에서 pH 10.0범위에서 1시간 이상 방치한 후에도 약 90% 이상의 $\alpha$-galactosidase 활성을 유지하였다. 또한 분리균이 생산하는 $\alpha$-galactosidase는 melibiose, raffinose와 stachyose와 같은 저당류를 가수분해 할 수 있으며 분해산물로 galactose를 방출하는 것으로 보아 $\alpha$-1,6 결합을 분해한 것으로 확인되었다.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
• /
• pp.67.1-67.1
• /
• 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)

• 약학회지
• /
• 제35권4호
• /
• pp.314-318
• /
• 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.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
• /
• pp.345.2-345.2
• /
• 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)