• Archives of Pharmacal Research
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• v.13 no.1
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• pp.1-4
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• 1990

Reaction of propane-1, 3-sultone with amines gave N-substituted aminosulphonnic acids 2a-i, Dehydration of 2a-c with $POCI_3$ gave the corresponding sultams 3a-c. Propane-1, 3-sultone 1 reacted with tertury amines to give the betaiene salts 4-11. 2-4-Dimethyl-1, 3-butadiene-1, 4-sultone 12 condensed with amines to give N-substituted-2, 4-dimethyl-1, 3-butadiene-1, 4-sultames 13a and 13b. The reaction of 3a, 13a with hydrazine hydrate gave acid hydrazides 3d or 13c. Compounds 3d, 13c reacted with isocyanates to yield urea derivatives 14a-c, 15a-c.

• Journal of the Korean Chemical Society
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• v.47 no.4
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• pp.345-353
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• 2003

The reaction of 6-chloro-3-methoxycarbonylmethylene-2-oxo-1,2,3,4-tetrahydroquinoxaline(5) or 3-methoxycarbonylmethylene-6-nitro-2-oxo-1,2,3,4-tetrahydroquinoxaline(6) with hydrazine hydrate gave 3-hydrazinocarbonylmethylene-2-oxo-1,2,3,4-tetrahydroquinoxalines(7, 8). The reaction of compound 7 or 8 with substituted benzaldehydes or heteroaromatic aldehydes afforded quinoxalines(9-14). Compounds showed the tautomerism between the enamine and methylene imine forms, and between the enamine, methylene imine and enaminol forms in dimethyl sulfoxide solution. The tautomer ratios were determined by the 1H NMR.

• Journal of the Korean Chemical Society
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• v.47 no.3
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• pp.241-249
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• 2003

The reaction of 3-(1-ethoxycarbonyl)ethyl-1,2-dihydro-2-oxoquinoxaline (8) with hydrazine hydrate gave 3-(1-hydrazinocarbonyl)ethyl-2-hydroxyquinoxaline (9). The reaction of compound 9 with substituted benzaldehydes and heteroaryl aldehydes afforded 2-hydroxyquinoxalines (10-12), respectively. The reaction of compound 9 with alkyl (ethoxymethylene)cyanoacetates and ethoxymethylenemalononitrile resulted in the intramolecular cyclization to give the 5-amino-1-[2-(3-hydroxyquinoxalin-2-yl)propanoyl]-pyrazoles (13), respectively. Compounds 10-13 showed the tautomerism between the lactam and lactim forms in dimethyl sulfoxide solution. The tautomer ratios were determined by the $^1H$ NMR. The herbicidal and fungicidal activities of the synthesized compounds were investigated.

• YAKHAK HOEJI
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• v.33 no.5
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• pp.290-295
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• 1989

2,6-Dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid methyl ester (1) was formylated to 2,6-dimethy-4-(3'-nitrophenyl)-5-formyl-1,4-dihydropyridine-3-carboxylic acid methyl ester (2) in 76% yield. At the elevated temperature, 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-monomethyl ester (3) was also converted into compound 2 in 46% yield. The compound 2 was reduced to 2,6-dimethyl-4-(3'-nitrophenyl)-5-hydroxymethyl-1,4-dihydropyridine-3-carboxylic acid methyl ester (4) in 91% yield. Compound 2 was reacted with triethyl phosphonoacetate to give 2,6-dimethyl-4-(3'-nitrophenyl)-5-(2-ethoxycarbonyl ethenyl)-1,4-dihydropyridine-3-carboxylic acid methyl ester (5) in 50% yield. Reaction between compound 2 and amines (methyl amine, ethylamine, methoxylamine, hydroxyl amine, phenyl hydrazine and 1-amino-4-methyl piperazine) gave six schiff bases 7a, 7b, 7c, 7e, 7f in 81%, 91%, 82%, 81%, 50% and 84% yield, respectively.

• Journal of the Korean Graphic Arts Communication Society
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• v.16 no.3
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• pp.1-13
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• 1998

Some photopolymer, poly(vinyl cinnamoyl acetate)(PVCiA) was synthesized by esterification of polymer(vinyl alcohol(PVA) with monochloroacetic acid, followed by reaction poly(vinyl monochloroacetate)(PVChA) and potassium cinnamate. When esterification of PVA with monochloroacetic acid was reacted in the dimethyl sulfoxide(DMSO), in the synthesis of PVChA, it is very good yield and the successive cinnamoyl acetoxyl esterification of PVCiA can be successfully synthesized. But PVCiA is low photosensitive polymer if not added photosensitizing dyes. Here, we synthesized photosensitizing dyes. trifluoromethylindol squarylium dye derivatives(TFSQ). Indolization of 3-trifluoromethylphenyl-hydrazine formed 4- and 6-substituted indoles, the rate of 4- and 6-substituted indoles is close to unity. Absorption's coefficient of 1,3-bis(4-trifluoromethyl-1,3,3-trimethylindol) squarylium dye(TFSQ) is 7.57$\times$10\ulcorner, PVCiA added with TFSQ(3%) was highly sensitized six times than not added.

• Natural Product Sciences
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• v.3 no.2
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• pp.89-99
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• 1997

Aminolysis, hydrazinolysis and alkylation of 4-methoxy and 4,9-dimethoxy-6-cyano-7-thione-5-methyl-7H furo [3,2-g] [1] benzopyridine (1 a-b) yielded 7N-substituted furobenzopyridine derivatives (2 a-e or the possible isomers 3 a-e and 4 a-b), (5 a,b and 6 a,b) and the ester (8 a,b). Hydrolysis of (la) with acetic acid gave the corresponding pyridone derivatives (7). Furobenzopyridinyl-7-thioacetyl hydrazide (9 a,b) have been prepared via alkylation of furobenzopyridine thione (1 a-b) with ethyl chloroacetate followed by condensation with hydrazine hydrate. Schiff base (11) was prepared by reacting (9a) with p. N,N-dimethyl aminobenzaldehyde in boiling ethanol. Treatment of (8a) with anthranilic acid gave the corresponding 7-substituted-4H-3,1-benzoxazine-4-one (10). We found that compound (11) increased bleeding, coagulating time, the total count of white blood cells, blood glucose level (cause hyperglycemia), enzymes (GOT, GPT) activities, concentration of urea and creatinine. On the other hand it decreased red blood cells number, haemoglobin content and haematocrite value.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.14
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• pp.5823-5828
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• 2015

Micronutrients in food have been found to have chemopreventive effects, supporting the conclusions from epidemiologie studies that consumption of fresh fruits and vegetables reduces cancer risk. The present study was carried out to evaluate the role of querctin (Q) and sodium gluconate (GNA) supplementation separately or in combination in ameliorating promotion of colon tumor development by dimethyl-hydrazine (DMH) in mice. Histopathological observation of colons in mice treated with DMH showed goblet cell dysplasia with inflammatory cell infiltration. This pathological finding was associated with significant alteration in oxidative stress markers in colon tissues and carcinoembryonic antigen (CEA) levels in plasma. Mice co-treated with GNA and Q showed mild changes of absorptive and goblet cells and inflammatory cell infiltration in lamina properia, with improvement in oxidative stress markers. In conclusion, findings of the present study indicate significant roles for reactive oxygen species (ROS) in pathogenesis of DMH-induced colon toxicity and initiation of colon cancer. Also, they suggest that Q, GNA or the combination of both have a positive beneficial effect against DMH induced colonic cancer induction in mice.

• Archives of Pharmacal Research
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• v.20 no.6
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• pp.620-628
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• 1997

6-Aryl-5-cyano-4-pyrimidinon-2-thione derivatives 1a-c reacted with ethyl iodide to give the corresponded 2-S-ethylpyrimidin-4-one-derivatives 2a-c. Compounds 2a-c was, in turn, reacted with hydrazine hydrate to give the sulfur free reaction products, 3a-c. These reaction products were taken as the starting materials for the synthesis of several newly synthesized heterocyclic derivatives. Reactions with several halogenated ketones, esters, chloroacetic acid and chloroacetamide give pyrimidotriazines 8,12 and 15 while their reactions with formic acid, acetic acid and carbon disulfide gave the corresponded triazolopyrimidines 17 and 21. The reaction with both acetyl acetone and ethylacetoacetate gave the corresponded 2-$(3^{I},5^{I}-dimethyl-1^{I}-pyrazoly$pyrimidine derivatives 20a-c and 24a-c respectively while the reaction with cinnamonitriles 25a-h afforded the corresponded aryl hydrazopyrimidines 27a-f. The structure of these reaction products were eatablished based on both elemental anlayses and spectral data studies.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.2
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• pp.487-492
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• 2012

Trace element zinc deficiency or excess is implicated in the development or progression of some cancers. The exact role of zinc in the etiology of colon cancer is unclear. To cast light on this question, an experimental model of colon carcinogenesis was applied here. Six week old rats were given sub cutaneous injections of DMH (30 mg/kg body weight) twice a week for three months and sacrificed after 4 months (precancer model) and 6 months (cancer model). Plasma zinc levels showed a significant decrease (p<0.05) at 4 months and a greater significant decrease at 6 months (p<0.01) as compared with controls. In the large intestine there was a significant decrease in tissue zinc levels (p<0.005) and in CuZnSOD, and alkaline phosphatase activity (p<0.05) in the pre-cancerous model and a greater significant decrease in tissue zinc (p<0.0001), and in CuZnSOD and alkaline phosphatase activity (p<0.001), in the carcinoma model. The tissue zinc levels showed a significant decrease in the small intestine and stomach (p<0.005) and in liver (p<0.05) in the cancer model. 87% of the rats in the precancer group and 92% rats in the cancer group showed histological evidence of precancerous lesions and carcinomas respectively in the colon mucosa. This study suggests that the decrease in plasma zinc, tissue zinc and activity of zinc related enzymes are associated with the development of preneoplastic lesions and these biochemical parameters further decrease with progression to carcinoma in the colon.

• Journal of fish pathology
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• v.20 no.3
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• pp.307-313
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• 2007

In this study, a QCM biosensor was made to detect Edwardsiella tarda (E. tarda) using a specific antibody. A 9 MHz AT-cut piezoelectric wafer layered with two gold electrodes of 5mm diameter had a reproducibility of 0.1 Hz in frequency response and was used as the transducer of the QCM biosensor. Self assembled layer (SAM) was conformed on a quartz crystal by treating with 3-mer-captopropionic acid (MPA) and activated with N-ethyl-N'-(3-dimethyl-aminopropyl) carbodiimide (EDC) and N-hydroxysuccinimide (NHS). The resulting NHS group was further converted to hydrazide by the reaction with hydrazine. Aldehyde group was introduced into the carbohydrate moiety of anti-E. tarda antibody by the reaction with periodic acid and was used to immobilise the antibody through the reaction with hydrazide group on the electrode surface. A baseline was established in the presence of phosphate-buffered saline (PBS) and a resonant frequency (F1) was measured. Sample was added to the sensor surface and second resonant frequency (F2) was measured after unbound substances were washed out with PBS several times. Finally, the frequency shift (ΔF) representing the mass change was calculated by subtracting F2 from F1. After adding the oxidized anti-E. tarda antibody to the electrode surface containing hydrazide group, frequency shift of 288.811.4 Hz (mean S.E) was observed, thus proving that considerable amount of antibody was immobilized. In the immunoassay test, the frequency shift of 1877.75 Hz, 580.67 Hz, 221.39 Hz, 7.671.83 Hz (mean S.E) were observed at doses of 1000, 500, 100, 50 g of bacterial cells, respectively. It was also demonstrated that the prepared sensor chip was stable enough to withstand repeated surface regeneration with 0.2 M Tris-glycine and 1 % DMSO, pH 2.3 more than ten times.