• Parasites, Hosts and Diseases
• /
• v.30 no.3
• /
• pp.191-200
• /
• 1992

A proteolytic enzyme was purified from the tissue extract of spargana (plerocercoids of Spirometra erinacei) by DEAE-Trisacryl M ion exchange chromatography and thiopropyl-sepharose affinity chromatography resulted in a 21-fold purification. The proteinase activity was assayed with a synthetic fluorescent substrate, carbobensoxy-phenylalanyl-7-amiso-4-trifluoromethyl-coumarin. SDS-polyacplamide gel electrophoresis of the purified materials revealed a single 28,000 dalton band. Inhibitor profiles of the band indicated that it belonged to cysteine endopeptidases. It exhibited identical pH curves with optimum at pH 5,5, and 50% activity from pH 4.7 to 8. It could completely degrade collagen chains to three identical products. It also showed some activity on hemoglobin. Furthermore, the band on immunoblots was reactive to the sera of sparganosis patients. These results suggest that the proteolytic enzyme belongs to cysteine proteinase which plays a role in the tissue penetration. Also it may be used as the antigen for diagnosis of active sparganosis.

• Polymer(Korea)
• /
• v.29 no.2
• /
• pp.216-220
• /
• 2005

A new type of polymer gel electrolyte was prepared from poly(ethylene glycol) diacrylate(PEGDA) and 1-butyl-3-methylimidazolium bis((trifluorornethyl) sulfonyl) amide$(BuMeIm^+Tf_2N^-)$ ionic liquid. The effect of the ionic liquid on ionic conductivity of the gel polymer electrolyte was investigated. It was observed that the gel polymer electrolyte having the ionic liquid exhibited higher ionic conductivity $(ca.\;10^{-3}S/cm)$ as well as electrochemical stability than that using organic solvent.

• The Korean Journal of Pesticide Science
• /
• v.3 no.1
• /
• pp.96-101
• /
• 1999

3-Trifluoromethylpyrazoles and 4-benzenecarbinolpyrazoles were prepared by the new synthetic methodologies, and their herbicidal effects were tested (in vivo) in the upland conditions and in the flooded paddy conditions for the purpose of the development of new herbicides. In upland conditions, most of the pyrazoles showed weak herbicidal effects at 4 kg/ha dosage in the post-emergence test, while no herbicidal effects in the pre-emergence test. In the flooded paddy conditions, some of the pyrazoles showed good herbicidal effects at a rate of 4 kg/ha, especially, 3-trifluoromethyl-4-(4-methoxybenzoyl)pyrazole showed the best herbicidal activity with good selectivity between rice and weeds. But other derivatives substituted with electron-donating groups such as dior trimethoxy and sulfides, and 4-benzenecarbinolpyrazoles showed weak herbicidal effects.

• Toxicological Research
• /
• v.13 no.4
• /
• pp.317-322
• /
• 1997

Acute delayed neurotoxicity of KH-502 [O.O-Diethyl O-(1-phenyyl-3-trifluoromethyl-5-pyrazoyl) thiophosphoric acid ester], an insecticide synthesized newly in Korea, was studied in White Leghorn hens. The doses were determined on the basis of preliminary $LD_{50}$ study. High, middle and low doses were determined to be 1123 mg/kg, 762 mg/kg and 518 mg/kg, respectively. The animals were pretreated with atropine (30 mg/kg) prior to administration of KH-502. The chemical was administrated at the first and 21st day of the study. As positive controls, animals were admlnistrated with triorthocresylphosphate (TOCP 1000 mg/kg and 500 mg/kg). Animals administrated with TOCP or KH-502 were sacrificed by perfusion-fixation at 21st and 42nd day of the study, respectively. The central and peripheral nerve tissues were routinely treated for microscopic observation. As results, eight, three, one, and one chickens died within 2 day after adminiatration with signs of cholinergic acute toxicity in high, middle low and TOCP dose-group (500 mg/kg), respectively. No abnormal clinical signs were observed in the survived chickens administrated with KH-502 in the duration of the study. The chickens in positive control groups showed ataxia and incoordination at the 14th day after administration of TOCP. From necropsy, macroscopic changes were not observed in all groups including positive control groups. Histopathologically, oxonal swelling with myelin loss, focal gliosis, distention around axonal space were observed in the spinal cords of the chickens administrated with TOCP 1000 mg/kg. The lesions were distinct in the dorsal and lateral funiculi of cervical spinal cord, in the lateral and ventral funiculi of thoracic spinal cord and in ventral funiculi of lumbosacral spinal cord. Axonal swelling and mlcrogliosis were infrequently observed in the chickens of other groups including negative control one. However, they were nonspecifically distributed in the spinal cords. In this study, we concluded that the new chemical, KH-502 did not have acute delayed neurotoxicity in White Leghorn hens.

• Korean Journal of Weed Science
• /
• v.9 no.3
• /
• pp.238-244
• /
• 1989

The experiment was carried out to evaluate the herbicidal properties of dithiopyr(3, 5-pyridine dicarbothioic acid-2-(difluoromethyl)-4-(2-methylpropyl)-6-(trifluoromethyl)-S,S-dimethyl ester). Weeding effect of dithiopyr was determined under various factors such as dosage, soil type, leaching amount, temperature, water depth, overflow time, and application time and method. Dithiopyr showed very high phytotoxic activity on most major annuals weeds, expecially Echinochloa crus-galli and Monochoria vaginalis. Excellent control of Echinochloa crus-galli was obtained at 0.04kg a.i./ha with preemergence application and 0.12kg a.i./ha with early post-emergence application (12 DAT ; Echinochloa crus-galli of 1.5 leaf stage). Weeding effect of dithiopyr decreased when applied at the soil surface 2days before transplanting. Soil type, leaching amount, temperature, water depth, overflow time did not affect the weeding effect.

• Bulletin of the Korean Chemical Society
• /
• v.31 no.1
• /
• pp.75-81
• /
• 2010

The reaction of N,N-diethyl carbamates of 1H-[1,2,3]triazolo[4,5-b]pyridin-1-ol (4-HOAt) 7, 3H-[1,2,3]triazolo[4,5-b]pyridin-3-ol (7-HOAt) 8, 1H-benzo[d][1,2,3]triazol-1-ol (HOBt) 9, 6-chloro-1H-benzo[d][1,2,3]triazol-1-ol (Cl-HOBt) 10, 6-(trifluoromethyl)-1H-benzo[d][1,2,3]triazol-1-ol ($CF_3$-HOBt) 11, and 6-nitro-1H-benzo[d][1,2,3]triazol-1-ol ($NO_2$-HOBt) 12 with morpholine and piperidine in $CH_3CN$ underwent acyl nucleophilic substitution to give the corresponding carboxamide derivatives. The reactants and products were identified by elemental analysis, IR and NMR. We measured the kinetics of these reactions spectrophotometrically in $CH_3CN$ at a range of temperatures. The rates of morpholinolysis and piperidinolysis were found to fit the Hammett equation and correlated with $\sigma$-Hammett values. The values were 1.44 - 1.21 for morpholinolysis and 1.95 - 1.72 for piperidinolysis depending on the temperature. The $Br{\phi}$nsted-type plot was linear with a $\beta_lg = -0.49 \pm 0.02$ and $-0.67 \pm 0.03$. The kinetic data and structure-reactivity relationships indicate that the reaction of 9-12 with amines proceeds by a concerted mechanism. The deviation from linearity of the correlation ${\Delta}H^#$ vs. ${\Delta}S^#$ and plot of $logk_{pip}$ vs. $logk_{morph}$ and $Br{\phi}$nsted-type correlation indicate that the reactions of amines with carbamates 7 and 8 is attributed to the electronic nature of their leaving groups.

• Archives of Pharmacal Research
• /
• v.23 no.4
• /
• pp.315-323
• /
• 2000

Syntheses of new analogues of oxathiin carboxanilide (UC84) and their antiviral activities were described. The heterocyclic carboxylic acids including oxathiins (4), thiazines (9) and dithiins (13) in which the methyl was replaced either by lipophilic trifluoromethyl- or bulky phenylgroup were synthesized starting from $\beta$-keto esters (5). Reaction of 4, 9 and 13 with thionyl chloride followed by treatment of the substituted aniline 22 gave the corresponding carboxanilides (24a~24f). The carboxanilides were subjected to Laweson's reagent the corresponding thiocarboxanilides (24g~24k). The antiviral activities of the synthesized compounds against human immunodeficiency virus type 1 (HIV-1), poliovirus type 1 (PV-1 ), coxsackie B virus type 3 (CoxB-3), vesicular stomatitis virus (VSV) and herpes simplex virus type 1 (HSV-1) were presented. The antiviral activity against HIV-1 of dithiin carboxanilide (24e) was similar with that of UC84 (24a). The corresponding thiocarboxanilides (24g~24k) showed higher inhibitory activity against HIV-1 than the carboxanilides (24a, 24b, 24d, 24e). The compounds in which ether the lipophilic trifluorormethyl substituents (24d, 24f, 24i ,24k) or bulky phenyl substituent is present in the heterocyclic compounds showed lower inhibitory activity than that of the methyl substituents is present in the compounds against the HIV-1. But the trifluoromethylated dithiin (24f) showed higher inhibitory activity against PV-1 and CoxB-3 virus than commercial antiviral agents, ribavirin (RV).

• KOREAN JOURNAL OF CROP SCIENCE
• /
• v.42 no.1
• /
• pp.68-78
• /
• 1997

Laboratory and greenhouse studies were conducted to determine differential sensitivities on absorption of $^{14}$ C-oxyfluorfen and the anatomical responses in wheat and barley to protoporphyrinogen oxidase-inhibiting herbicides [oxyfluorfen (2-chloro-1- (3-ethoxy -nitrophen-oxy)-4-(trifluoromethyl) benzene, acifluorfen(5-[2-chloro-4-(trifluoromethyl) phenoxy]-2-nitro-benzoic acid), bifenox(methyl-5-(2, 4-dichlorophenoxy)-2-nitrobenzoate) and oxadiazon(5-tert-butyl-3-(2, 4-dichloro-5-isopropoxyphenyl)-1, 3, 4-oxadiazol-2-one)]. I$_{50}$ value of the tolerant wheat cultivars to oxyfluorfen was about 10$^{-4}$ , whereas that of the susceptible barley cultivars was about 10$^{-6}$ M, showing significant difference between the two groups. When foliage were applied with acifluorfen, bifenox or oxadiazon, the oxyfluorfen-tolerant wheat showed less decreased in shoot fresh weight and chlorophyll content than the susceptible barley. Also, when soil-applied with these herbicides test plants showed similar tendency in foliar application. Electrolyte leakage from the tissue treated with these compounds was the more influenced in the barley than the wheat. Malondialdehyde(MDA) production as index of lipid peroxidation was greater in the barley than the wheat by treatment of these compounds. Therefore, the differential sensitivities of wheat and barley to protoporphyrinogen oxidaseinhibiting herbicides was showed by our greenhouse and in vitro experiment. The absorption rates of $^{14}$ C-oxyfluorfen were higher in the barley than the wheat. And this tendency was showed appararitly difference by increase of treatment durations. After the oxfluorfen and oxadiazon treatment, the tolerant wheat did not show the structural damage in leaf surface, but the susceptible barley was damaged in the leaf waxy layer. However, the acifluorfen and bifenox treatment showed no difference between wheat and barley. The anatomical changes by these compounds treatment were not observed in the tolerant wheat but epidermal cell and mesophyll cell were highly broken in the susceptible barley.

• Korean Journal of Weed Science
• /
• v.11 no.1
• /
• pp.26-31
• /
• 1991

The effects of varying concentrations and durations of ethalfluralin (N-ethyl-N-(2-methyl-2-propenyl)-2, 6-dinitro-4-(trifluoromethyl) bezenmine) treated on oat(Avena sativa L.) cell division, cell enlargement, protein synthesis and histology were studied. After 6hr treatment, all concentrations(1${\times}$10^{-6}M to $1{\times}10^{-3}$) of ethalfluralin arrested completely metaphase in the cell division study. The oat coleoptile inhibition of straight-growth test were used to determine the influence of ethalfluralin on coleoptile growth. A range of all concentrations($1{\times}10^{-8}$M to $1{\times}10^{-3}$M) treatment did affect cell enlagement significantly. The $1{\times}10^{-6}$M to $1{\times}10^{-3}$ M concentrations reduced approximately over 50% cell enlargement. Protein incorporation study showed that all concentrations($1{\times}10^{-6}$M to $1{\times}10^{-3}$M) were not affected in protein synthesis. To investigate histological effects, the oats were treated for 24hr with $1{\times}10^{-7}$M. The longitudinal section cells, in the treated oat root tips were appeared to be enlarged and also showed lacking cytoplasm, multinucleate or abnormal cells compare with untreated roots.

• Bulletin of the Korean Chemical Society
• /
• v.28 no.12
• /
• pp.2449-2453
• /
• 2007

L-[18F]FMAU ([18F]1b) was prepared from the precursor 2-O-[(trifluoromethyl)-sulfonyl]-1,3,5-tri-Obenzoyl- α-L-ribofuranose, by coupling the radioactive fluoro-sugar with the corresponding silylated thymine in 4 steps. The final products, including the α and β anomers, were purified using reverse phase HPLC with an appropriate solvent (5% CH3CN/H2O) at a flow rate of 3.0 mL/min. The total elapsed time of synthesis was about 180-200 min from EOB. The α/β anomeric ratio of the compounds was about 1:9, and the radiochemical purity of the product (β-form) was >98% with decay-corrected yields of 25-35%. All radioactive samples were confirmed using co-injection with pure non-radioactive analogues in every step. In the cellular uptake in vitro test of herpes simplex virus-thymidine kinase (HSV1-TK) gene expressed cells, the percent uptake of injected dose (%ID) of L- and D-FMAU was 37.28 and 65.86, respectively after 240 min incubation. However, the relative uptake (MCA-TK/MCA cellular uptake ratio) of L-FMAU was higher than that of D-FMAU (%ID of L-FMAU, 0.36 and D-FMAU, 0.93 after 240 min incubation in MCA cells). This means that L-FMAU will show better specific HSV1-TK gene expressed cell uptake for selective HSV1-TK gene imaging.