• Archives of Pharmacal Research
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• v.15 no.3
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• pp.224-228
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• 1992

Arylhydrazones of diethylacetondicarboxylate 3 was treated with formaldehyde to give 1 aryl-4, 5, 6-trihydropyridaine derivatives 4a-f Cyclization of compound 4a-f by hydroxylamine afforded [3, 4d] 1, 3, 4, 5-tetrahydropyridazine derivatives 5a-f. Also cyclization of compound 4c with semicarbazide gave 1-amidopyrazolo-5-one-1-aryl-3-carboxypyridazine 6. On the other hand compounds 3 reacted with ethylorthoformate to give diethyl-1, 4-dihydro-1-arylpyridazine-4one-2.5 dicarboxylate 7, which on treatment with hydrazine. Semicarbazide and thiosemicarbazide gave pyridazine, amido and thioamido derivatives. The spectral and antimicrobial data of these compounds 1-8 were studied.

• Natural Product Sciences
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• v.19 no.1
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• pp.8-14
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• 2013

The inhibitory effect and the structure-activity relationships of luteolin and its related derivatives isolated from Taraxacum mongolicum against MAO activities were investigated. The activity-guided isolation of extract from Taraxacum mongolicum led to the isolation of three flavonoids, luteolin, diosmetin, and luteolin-7-glucoside, a polyphenol, chlorogenic acid, a tyrosine and a uridine. The inhibitory activities of luteolin and its related derivatives against MAOs activities are dependent on their molecular structures. The presence of the phenolic hydroxy group at para-position is the active site for MAO-A inhibition as well as of MAO-B. The methoxy group has no potential on MAO-A inhibition. An additional phenolic hydroxy group at the ortho-position alleviates about 4-fold MAO-A inhibitory activity of phenolic hydroxy group at para-position. A carboxylic group seems to be critical for DBH inhibition and has no effects on MAO.

• Journal of the Korean Chemical Society
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• v.55 no.6
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• pp.988-993
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• 2011

Cyclodehydration of 6-amino-5-cyano pyrimidine derivative (2) afforded pyrimidoisoindole derivatives (3). Compound (3) reacted with carbethoxymethylene derivative to give pyridopyrimidine derivatives (5a,b). Compound (3) was also reacted with formamide to give the corresponding pyrimidopyrimdine derivatives (6) that condensed with benzaldehyde to give Schiff's base (7). Refluxing of compound (3) with triethyl orthoformate afforded compound (8) that cyclized with ammonium hydroxide giving the same compound (6). Compound (8) cyclized with hydrazine hydrate giving compound (9) which also cyclized with triethyl orthoformate affording compound (10). Diazotization of compound (3) led to the formation of triazinopyrimidine derivative (11). Cyclization of compound (11) upon treatment with hydrazine hydrate afforded compound (12). Compound (15) was prepared from reaction of compound (3) and ethylenediamine in presence of carbon disulfide. The behaviour of compound (15) toward benzoyl chloride, triethyl orthoformate, nitrous acid and/or carbon disulfide was also described. All proposed structures were supported by elemental analyses, spectroscopic data and some of the new products showed antimicrobial activity.

• Bulletin of the Korean Chemical Society
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• v.33 no.6
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• pp.1907-1912
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• 2012

Ailanthoidol showed a strong $anti$-inflammatory effect in a previous result. Ailanthoidol derivatives were prepared for the $anti$-inflammatory test using Sonogashira coupling, iodine induced cyclization and Wittig reaction. $Anti$-inflammatory effects of the prepared ailanthoidol derivatives were examined in lipopolysaccharide (LPS)-stimulated RAW 264-7 macrophages. The results showed that some ailanthoidol derivatives inhibited significantly the production of inflammatory mediator nitric oxide.

• YAKHAK HOEJI
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• v.59 no.2
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• pp.55-58
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• 2015

A series of N-substitutedaryl-3-phenylpropanamide derivatives were synthesized and their inhibitory activities on LPS-induced NF-$1{\kappa}B$ transcriptional activity on RAW 264.7 cells were evaluated. Cl substituted derivatives (1e, 1f) have shown more potent activities than parent hit compound KL-1156.

• Bulletin of the Korean Chemical Society
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• v.17 no.4
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• pp.342-347
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• 1996

Voltammetric determination of phenol derivatives, such as phenol, o-, m-, and p-cresols was studied with a β-Cyclodextrin (β-CD) modified-carbon paste electrode composing of the graphite powder and Nujol oil. Phenol derivatives were chemically deposited via the complex formation with β-CD by immersing the CME into a sample solution. The resulting surfaces were characterized with cyclic and differential pulse voltammetry. Treating the CME with 1 M nitric acid for five sec after a measurement could regenerate the electrode surface. Linear sweep and differential pulse voltammograms were recorded for the above system to optimize the experimental parameters for analysing the phenol derivatives. In this case, the detection limit for phenols was 5.0×10-7M for 25 min of the deposition time with differential pulse voltammetry. The relative standard deviation was ±5.2% of 3.0×10-6M (four repetitions). The interference effect of the following organic compounds was also investigated; Bezoic acid, hippuric acid, o-, m-, and p-methylhippuric acid. Adding the organic compounds into the sample solution reduces the peak current of the phenols to about 25%.

• Archives of Pharmacal Research
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• v.12 no.4
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• pp.259-262
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• 1989

The reaction of the sodium salts of 4-methoxy and 4, 7-dimethoxy 6-hydroxy benzofuran-5-carboxylic acid with ethyl chloroformate yields the corresponding dicarbethoxy derivatives. The N-substituted amides were obtained by treating the latter compounds with amines. The corresponding hydrazides were synthesized by the reaction of hydrazine hydrate on the dicarbethoxy derivatives which spontaneously cyclized to 5-substituted-2, 3- dihydro-1, 3, 4, -oxadiazol-2-one. Also the reaction with phenyl hydrazine has been studied. The dicarbethoxy derivatives and N-substituted amides were tested against Gram positive and Gram negative bacteria in vitro. Most of the compounds posses moderate or slight activity against Gram positive bacteria.

• Journal of Life Science
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• v.8 no.4
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• pp.395-399
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• 1998

Neurokinin A(NKA) and its derivatives ([Nle$^{7}$NKA,[Leu$^{7}$NKA] were synthesized by solid phase peptide synthesis method using Fmoc-TFA strategy and their smooth muscle contractile activities were measured to examine the structural effect of alkyl group at the 7th amino acid NKA on the smooth muscle contractile activity. The smooth muscle contractile activity. The smooth muscle contractile activities of [Nle$^{7}$]NKA and [Leu$^{7}$]NKA were only 5.64% and 1.55%, respectively when compared with NKA. This result suggested that the more three dimensional structure of th 7th amino acid as well as the whole message segment of NKA would be necessary to show the biological activity.

• Natural Product Sciences
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• v.14 no.2
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• pp.131-137
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• 2008

From the 70% EtOH extract of the roots of Astragalus membranaceus (Leguminosae), eleven flavonoid derivatives and a lignan, were isolated and identified as liquiritigenin (1), daidzein (2), formononetin (3), sophorophenolone (4), calycosin (5), methylnissolin (6), isomucronulatol (7), isomucronulatol 7-O-glucoside (8), methylnissolin 3-O-glucoside (9), calycosin 7-O-glucoside (10), (+)-syringaresinol O-${\beta}$-D-glucoside (11), and isomucronulatol 7,2'-di-O-glucoside (12), by spectroscopic methods. This is the second report of the isoflavonoid derivatives sophorophenolone (4) and isomucronulatol 7,2'-di-O-glucoside (12) from a natural source, as well as the first report of compounds liquiritigenin (1), daidzein (2) and (+)-syringaresinol O-${\beta}$-D-glucoside (11) from the species A. membranaceus.

• Bulletin of the Korean Chemical Society
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• v.23 no.10
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• pp.1425-1446
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• 2002

An efficient procedure for the synthesis of 6,7-dichloro-5,8-phthalazinedione (4) was developed in 49% overall yield via chloroxidation of 5,8-diaminophthalazine (8). And a series of its derivatives, 7-pyridinium-5,8-phthalazinedione-6-oxide (9), 6-chloro-7-phenylamino-5,8-phthalazinedione (10), 6,6-dimethoxy-6H-2,3,6b,11-tetraazabenzo[a]fluoren-5-one (11a), and 6,6-diethoxy-6H-2,3,6b,11-tetraazabenzo[a]fluoren-5-one (11b) have been synthesized.