• Bulletin of the Korean Chemical Society
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• 제23권6호
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• pp.787-788
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• 2002

• 약학회지
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• 제16권2호
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• pp.97-107
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• 1972

Thirty-three Mannich bases of 2,2'-methylene bis(3,4,6-trichlorophenoxyacetic acid) were synthesized as potential antimicrobial agents and tested against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Trichophyton rubrum, Microsporum gypseum, Epidermophyton floccosum, Aspergillus niger and Aspergillus oryzae in vitro. It was found that: 1) Compounds 24 and 22 were active against Staphylococcus aureus and Bacillus subtilis at the concn. of 1 $\mu$g/ml respectively; 2) Compounds 9 and 29 were active against Trichophyton rubrum at the concn. of 2 $\mu$g/ml respectively; 3) Compouns 9 and 30 were active against Microsporum gypseum at the concn. of 2 $\mu$g/ml respectively; 4) Compounds 6,9,13,15,21,28,29,31,33 and 34 were active against Epidermophyton floccosum at the concn. of 1 $\mu$g/ml respectively; 5) Compounds 6,9,18 and 28 were active against Aspergillus niger and Aspergillus oryzae at the concn. of 1 $\mu$g/ml respectively.

• Archives of Pharmacal Research
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• 제14권3호
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• pp.266-270
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• 1991

Synthesis of C-(2-furyl)-N-(4-nitrophenyl)methanohydrazonyl bromide 2 is described. Treatment of 2 with uncleophiles affords the corresponding substitution products 3-7. Also, compound 2 reacts with selenocyanate anion and thiocyanate anion and give the corresponding selenadiazoline and thiadiazoline 8 and 9, respectively. Moreover, reaction of 2 with enolates of various active methylene compounds afforded the pyrazole derivatives 17-20.

• Archives of Pharmacal Research
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• 제20권5호
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• pp.507-509
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• 1997

Several new spiro compounds were synthesized via one-pot ternary condensation of isatin, malononitrile and each of thiobarbituric acid, barbituric, 3-methyl-pyrazolin-5-one, 1-phenyl-3-methyl-pyrazolin-5-one, acetylacetone, benzoylacetone, ethyl acetoacetate, phenacyl cyanide or ethyl-cyanoacetate dimer. Structures and reaction mechanisms were reported and supported via a second synthetic route.

• Archives of Pharmacal Research
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• 제18권1호
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• pp.51-55
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• 1995

A facile convenient syntheses of the titled compounds, via reacting the precusor 2-amino-2-(pentane-2, 4-dion-3-yithio)-6-phenylpyrimidine-5-carbonitrile (1) with nitrogen nucleophiles and with the carbanions of some active methylene compounds, is reported. Chemical and spectroscopic evidence of the newly syntheised compounds are described.

• 대한화학회지
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• 제55권6호
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• pp.1000-1006
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• 2011

A systematic study of Knoevenagel reaction and Nazarov cyclization was made on variety of less reactive carbonyl compounds such as ${\beta}$-ketoesters, 1,3-diketones and cyclic active methylene compounds using $Yb(OTf)_3$ as the catalyst. Recycling study confirms reusability of the catalyst without much loss of activity.

• Archives of Pharmacal Research
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• 제13권4호
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• pp.314-318
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• 1990

2-Bromo (2'-benzofury)gloxal-2-aryhydrazones I reacted with nucleophiles displacing the bromide. Treatment of I with active methylene compounds yield the pyrazole derivatives VIII-XI. Compounds XII-XIV reacted with hydrazine to give pyrazolo (3, 4-dipyridazine derivative XIV-XIV. The structures of the products were assigned and confirmed on the basis of their elemental analysis and spectral data.

• Archives of Pharmacal Research
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• 제17권5호
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• pp.298-303
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• 1994

4-Arylazo-1H-pyrazol-3, 5-idimines 1a-c reacted with bromomalononitrile (2) to yield the corresponding imidazo[1, 2-b]pyrazoles 3a-c. The latter reacted with some active methylene compounds and with .alpha.-cinnamonitriles to afford the corresponding pyrazoloimidazopyridines 6, 8, 9 and 15, respectively. Compounds 3 reacted with each of formic acid, formamide, trichlo-roacetonitrile and with guanidine to yield the corresponding pyrazoloimidazopyrimidines 16-19 respectively.

• 생명과학회지
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• 제24권3호
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• pp.234-241
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• 2014

용규(Solanum nigrum)에 함유된 여러 성분 중 항암 활성이 있는 물질을 분리 및 규명하고자 용규를 MeOH로 추출하고 이 추출물을 $CH_2Cl_2$, EtOAc, n-BuOH, $H_2O$로 유기용매 계통분획 하였다. 이 분획물 중 $H_2O$ 획분이 가장 뛰어난 세포 독성 효과를 보였으며 이를 다시 용매별($H_2O$, 40% MeOH, 60% MeOH, MeOH)로 Diaion HP-20 column chromatography하여 4개의 fraction으로 나누었다. 이 fraction 중 $H_2O$ fraction에서 가장 뛰어난 세포 독성효과를 보였으며 몇 차례의 column chromatography를 행하여 얻어진 활성 획분을 GC-MS 및 FAB-MS 분석하였다. 분자량이 416이었으며 GC-Mass를 통하여 library search를 행한 결과 분자식 $C_{28}H_{48}O_2$인 Des-N-26-methylenedihydrotomatidine으로 확인되었다. Des-N-26-methylene-dihydrotomatidine과 비슷한 구조를 가지고 있는 tomatine과 tomatidine의 HT29 세포에 대한 세포독성효과를 확인한 결과, tomatine보다는 활성이 낮았으나 tomatidine 보다는 40 ${\mu}g/ml$ 이상의 농도에서 높은 세포독성 효과를 나타내었다. Des-N-26-methylene-dihydrotomatidine은 지금까지 학계에 보고되어 있지 않은 물질로, 본 연구에서 최초로 용규에서 Des-N-26-methylene-dihydrotomatidine을 분리하였고, 암세포에 대한 세포 독성 효과를 보고하였다. Des-N-26-methylene-dihydrotomatidine의 정상세포에서의 세포 독성 및 작용 기전 등의 추가 연구를 통해 천연 생리 활성 물질 소재로 활용 가능할 것으로 사료된다.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.256.3-257
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• 2003

The bioactivity-guided fractionation of an active methylene chloride extract of the sclerotium of Poria cocos led to the isolation of compounds 1-5. These compounds were tested in the human colon carcinoma and human breast carcinoma cell lines, compounds 3, 4, and 5 exhibited IC50 values of 10.8, 15.4, and 5.1 $\mu\textrm{g}$/$m\ell$ against human colon carcinoma cell line. In addition, compounds 3, 4 and 5 showed moderate activities as inhibitors of Topoisomerase I and all compounds were inactive in the Topoisomerase II inhibition.