• Bulletin of the Korean Chemical Society
• /
• v.23 no.6
• /
• pp.787-788
• /
• 2002

• YAKHAK HOEJI
• /
• v.16 no.2
• /
• pp.97-107
• /
• 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
• /
• v.14 no.3
• /
• pp.266-270
• /
• 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
• /
• v.20 no.5
• /
• pp.507-509
• /
• 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
• /
• v.18 no.1
• /
• pp.51-55
• /
• 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.

• Journal of the Korean Chemical Society
• /
• v.55 no.6
• /
• pp.1000-1006
• /
• 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
• /
• v.13 no.4
• /
• pp.314-318
• /
• 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
• /
• v.17 no.5
• /
• pp.298-303
• /
• 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.

• Journal of Life Science
• /
• v.24 no.3
• /
• pp.234-241
• /
• 2014

To identify and isolate anticancer active compounds from Solanum nigrum, S. nigrum was extracted with MeOH and then fractionated with various organic solvents ($CH_2Cl_2$, EtOAc, n-BuOH, and $H_2O$). The cytotoxic effects of the MeOH extracts from S. nigrum and its organic solvent-soluble fractions were also tested in HT29 cells. All the MeOH extracts of S. nigrum and its organic-solvent extracts induced cytotoxicity in the HT29 cells. Among the extracts, $H_2O$ was the most effective. The $H_2O$ extract was purified further by repeated silica gel, Sephadex LH-20, Diaion HP- 20, and RP-18 column chromatography. An active anticancer compound, Des-N-26-methylene-dihydrotomatidine, was isolated with a molecular weight of 416 and a molecular formula of $C_{28}H_{48}O_2$. Analysis of the cytotoxic effects of Des-N-26-methylene-dihydrotomatidine on the HT29 cells compared to those of tomatine and tomatidine are similar in its structure, is higher than tomatidine above the 40 ${\mu}g/ml$ concentration, but lower than tomatine. This is the first study to describe the anticancer activity of Des-N-26-methylene-dihydrotomatidin, isolated from S. nigrum. Des-N-26- methylene-dihydrotomatidine seems to have potential as a natural bioactive compound.

• Proceedings of the PSK Conference
• /
• 2003.04a
• /
• pp.256.3-257
• /
• 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.