• Environmental Mutagens and Carcinogens
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• v.21 no.2
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• pp.128-134
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• 2001

Single cell gel electrophoresis (SCGE) assay, also called comet assay, is a rapid and sensitive method to detect DNA damage in single cell level. To evaluate the DNA damage of lymphocytes of pesticides sprayers, SCGE assay was carried out for 50 pesticides sprayer and 58 control subjects. They were interviewed with structured questionnaire to get the information about the kinds and amount of pesticide. Insecticides and fungicides were predominant among pesticides. Major components of pesticides were organophosphorus, organosulfate, cartap, carbamates, and triazole. Sprayed pesticides were classified into two groups. Group I included organophosphorus, organoarsenic, organotin, tetrazine, triazole and gramoxone, which were known to cause DNA damages. Group II pesticide were carbamates, surfactants, organosulfates, etc., which were not found as DNA damaging agents in scientific documents. Olive tail moments of 100 lymphocytes were measured by KOMET 3.1 program for each person. The means of tail moments were compared between farmers exposed to pesticides and control subjects. Farmers showed higher tail moments than control subjects (2.07$\pm$1.40 vs 1.53$\pm$0.77, p<0.05). The means of tail moments also were compared among group I sprayers (n=36), group II sprayers (n=24) and, control subject, and the means or tail moments were 3.4s$\pm$3.2o, 2.66$\pm$2.20 and 1.53$\pm$0.77 respectively. The difference between means of group I sprayers and controls was statistically significant (p<0.05). In conclusion, this study showed higher DNA damage in farmers exposed to pesticides than control subjects, and comet assay could be useful as a biological monitoring method of genotoxic pesticides for farmers.

• Korean Journal Plant Pathology
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• v.13 no.4
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• pp.210-214
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• 1997

The experiment was conducted to obtain basic informations on the effects of key environments and fungicides on the sporulation, conidial germination and hitial growth of the hyphae of grape powdery mildew fungus Uncinula necator. Maximum sporulation occurred at RH 75~96% in vitro adiusted with sulfuric acid solution. Conidial germination and initial growth of the hyphae were better at 5% water agar than distilled water, and best at $26^{\circ}C$ and pH 5.0 of the substrates. Germination occurred equally well at light intensity of below 100 lux or dark condition, which was better at water agar supplemented with leaf extract 30% than pure water agar. The water agar supplemented with triazole fungicides reduced conidial germinations and initial growth of the hyphae signifcantly, in proportion to the increase in concentration of the fungicides, but the maguitude of reduction depended on the fungicides. Particularly in myclobutanil, reduction rate was very low as increased in concentration.

• Bulletin of the Korean Chemical Society
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• v.33 no.7
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• pp.2193-2199
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• 2012

A series of novel polytriazoleimides were prepared from various aromatic dianhydrides and a new kind of 1,2,3-triazole-containing aromatic diamine synthesized by the Cu (I)-catalyzed 1,3-dipolar cycloaddition reaction in DMAc, and characterized by FT-IR, $^1H$-NMR, XRD, DSC and TGA techniques. The results show the polytriazoleimides are soluble in most of strong polar solvents and have inherent viscosity values of 0.51-0.62 dL/g(DMAc). The polytriazoleimide films exhibit a tensile strength of 62.3-104.5 MPa and an elongation at breakage of 4.0-8.1%, a glass transition temperature ($T_g$) of $257-275^{\circ}C$, a decomposition temperature (at 5% weight loss) of $350-401^{\circ}C$ in $N_2$ atmosphere, and a dielectric constant of 2.47-3.01 at 10 MHz, which depend on the structure of the polymers. The polytriazoleimides perform good resistance to acid and alkali solution.

• Journal of the Korean Chemical Society
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• v.54 no.6
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• pp.737-743
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• 2010

Coupling of 5-amino-1,3-diaryl-pyrazoles 1a-c with diazonium salts of different aryl amines gave a series of novel 1,3-diaryl-5-amino-4-arylazopyrazoles 3a-l. Such compounds could be also obtained by reaction of 5-amino-1,3-diaryl-4-nitroso- 1H-pyrazoles 2a-c with different aryl amines in alkaline medium. Oxidation of azo derivatives 3a-l with cupric acetate, in dimethyl formamide and stream of air, gave 2,4,6-triaryl-2,4-dihydropyrazolo [4,3-d]-1,2,3-triazoles 4a-l. and the fluorescence properties of the cyclic triazoles were studied. Diazotization of 5-amino-1,3-diaryl-1H-pyrazoles 1a-c by sodium nitrite in ortho-phosphoric acid followed by coupling with some aryl amines gave o-aminoazo compounds 5a-f. Cyclisation of compounds 5a-f in pyridine and cupric acetate gave the corresponding triazoles 6a-f. The coupling of compounds 6a-f with different aryl diazonium salts gave compounds 7a-j. The synthesized dyes were applied to polyesters as disperse dyes and the fastness properties were evaluated.

• Bulletin of the Korean Chemical Society
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• v.26 no.5
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• pp.719-728
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• 2005

A novel 2-amino-4-(8-quinolinol-5-yl)-1- (p-tolyl)-pyrrole-3-cabonitrile (2) was obtained by the reaction of 2-[2-bromo-1-(8-hydroxyquinolin-5-yl)-ethylidene]-malononitrile (1) with p-toluidene. The new synthon compound (2) could be annelated to the corresponding pyrrolo[2,3-d]pyrimidines (4, 6, 7, 26-28), triazolo[1,5-c]pyrrolo[3,2-e]pyrimidines (10, 29, 30), pyrrolo[2,3-c]pyrazoles (11-15), pyrrolo[1,2-a]pyrrolo[3,2-e] pyrimidine (17) and imidazo[1,2-c]pyrrolo[3,2-e]pyrimidines (18-25) via the reaction with some reagents such as acetic anhydride, formamide, triethyl orthoformate, hydrazine hydrate, hydroxylamine, ethylenediamine, carbon disulfide and phosphorus oxychloride. Chemical and spectroscopic evidences for the structures of these compounds are presented. The antifungal and antibacterial activity of the newly synthesized comounds were evaluated.

• Bulletin of the Korean Chemical Society
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• v.31 no.12
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• pp.3684-3692
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• 2010

A series of azole-containing piperazine derivatives have been designed and synthesized. The obtained compounds were investigated in vitro for their antibacterial, antifungal and cytotoxic activities. The preliminary results showed that most compounds exhibited moderate to significant antibacterial and antifungal activities in vitro. 1-(4-((4-chlorophenyl) (phenyl)methyl)piperazin-1-yl)-2-(1H-imidazol-1-yl)ethanone and 1-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)-2-(2-phenyl-1H-imidazol-1-yl)ethanone gave remarkable and broad-spectrum antimicrobial efficacy against all tested strains with MIC values ranging from 3.1 to $25\;{\mu}g/mL$, and exhibited comparable activities to the standard drugs chloramphenicol and fluconazole in clinic. Moreover, 2-((4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)methyl)-1H-benzo[d]imidazole was found to be the most effective in vitro against the PC-3 cell line, reaching growth inhibition values (36.4, 60.1 and 76.5%) for each tested concentration: $25\;{\mu}g/mL$, $50\;{\mu}g/mL$ and $100\;{\mu}g/mL$ in dose-dependent manner. The results also showed that the azole ring had noticeable effect on their antimicrobial and cytotoxic activities, and imidazole and benzimidazole moiety were much more favourable to biological activity than 1,2,4-triazole.

• Bulletin of the Korean Chemical Society
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• v.33 no.9
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• pp.2985-2990
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• 2012

New thiazoline derivatives 7a-c, and thiophenes 9a-c linked to indole moiety were easily prepared via the reaction of the acrylamide derivative 3 with phenacyl bromides 4a-c, depending on the reaction conditions. In addition, the reaction of compound 3 with hydrazonoyl chlorides 11a-f afforded a series of 1,3,4-thiadiazole derivatives 13a-f. Moreover, coupling of 3-(3-methyl-1H-indol-2-yl)-3-oxopropanenitrile (2) with the diazonium salts of 3-phenyl-5-aminopyrazole 16 or 3-amino-1,2,4-triazole 17 gave the corresponding hydrazones 18 and 19, respectively. Cyclization of the latter hydrazones yielded the corresponding pyrazolo[5,1-c]-1,2,4-triazine and 1,2,4-triazolo[5,1-c]-1,2,4-triazine derivatives 20 and 21, respectively. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, $^1H$ NMR and mass spectral data. All the synthesized compounds were tested for in vitro activities against certain strains of fungi such as Aspergillus niger, Aspergillus nodulans, Alternaria alternate. Compounds showed marked inhibition of fungal growth nearly equal to the standards.

• Journal of the Korean Chemical Society
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• v.64 no.1
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• pp.7-18
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• 2020

An efficient and facile procedure has been developed for the synthesis of novel bichalcone derivatives (4a, 4b). The key step contains the solvent-free aldol synthesis of bichalcones based on quinones. Bichalcones (4a, 4b) were used as precursors for the synthesis of some interesting heterocyclic compounds like, diazepines (5a, 5b), pyrazolo-pyrimidines (7a, 7b), and pyrazoline derivatives (8a, 8b). Moreover, new thioxopyrimidine derivatives (9a, 9b) were furnished and used as a functionalizing agent to produce the triazole-pyrimidines (11, 12) and the carbonitrile derivative (14). All the synthesized compounds were fully characterized using physical and spectral data like, FT-IR, ¹H NMR, ¹³C NMR, and MS. Bichalcones (4a, 4b) and diazepines (5a, 5b) were screened for their anticonvulsant activity, where compounds (4a, 5a, and 5b) revealed potent anticonvulsant activity compared to diazepam. On the other hand, some of the prepared compounds were screened for their antiproliferative activity and they showed significant cytotoxic effects on most of the cancer cell lines with regard to broad spectrum antitumor activity.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.160-160
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• 1996

$\beta$-Lactam계 항생제 내성균의 문제를 해결할 수 있는 $\beta$-lactamase억제제의 개발을 위해서, cephalosporinase에 특히 높은 억제활성을 갖는 새로운 6-exomethylene penamsulfones 화합물을 합성하였다. Dibromopenamsulfone과 thioalkyl triazole-4-carboxaldehyde을 반응시키고, acetic anhydride와 Zn으로 처리하여 E-form과 Z-form의 6-exomethylene penam sulfones을 합성하였다. 이것을 AlCl$_3$으로 deprotection시킨 후, NaOH로 처리하여 6-exomethylene penamsulfone의 Na-salt form으로 목적물질을 합성하였다.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1997.04a
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• pp.71-71
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• 1997

$\beta$-lactamase를 생성하는 균들이 $\beta$-lactam계 항생제를 분해하여 불활성화 시키므로 이를 해결하기 위하여 그 효소에 대하여 억제활성을 나타내는 새로운 6-exomethylenepenamsulfone화합물들을 합성하였다. Dibromopenamsulfone과 heterocyclic ring을 함유한 thioethyl triazole-4-carboxaldehyde를 반응시키고, acetic anhydride와 Zn으로 처리하여 E-form과 Z-form의 6-exomethylene penmsulfones을 합성하였다. 이것을 AlCl$_3$로 처리하여 deprotection시킨 후, NaHCO$_3$로 처리하여 6-exomethylene penam sulfones의 Na-salt의 형태로 목적물질을 합성하였다.