• 한국응용과학기술학회지
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• 제14권2호
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• pp.93-102
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• 1997

Isothiazoline derivatives is widely used to food, medical drug and industrial goods, cosmetics etcs, and it makes to restrain and to sterilize a breeding of microbe as a preservative and a sterilizing agent. It differs with the raw material of paraoxybenzoic acid derivatives or imidazolydinyl urea to be in use at present, on the efficacy and effect, and has various characteristics. This synthesis makes 3,3'-dithiodipropionic chloride to add a thionyl chloride in 3,3'-dithiodipropionic acid, and 3,3'-dithiodipropionic methyl amide makes to synthesize in a reflux reaction the mono methyl amine to 3,3'-dithiodipropionic chloride. And last synthesis becomes to make chlorination-cyclization molecule doing a reflux reaction in the temperature of $90{\sim}100^{\circ}C$ to mix excessively thionyl chloride and ethylene dichloride to 3,3'-dithiodipropionic methyl amide. The last synthesis material has got in the mixture of 5-chloro-2-methyl-4-isothiazoline-3-one and 2-methyl-4-isothiazoline-3-one, and it is so-called isothiazoline derivatives. The purification of isothiazoline derivatives makes to fuse in ethyl acetate, and makes to decolorize and to deodorize in recrystallization. This experiment has been in synthesis and purification of isothiazoline derivatives, and has tried to measure on the antisepsis and sterilization function of microbe according to pH or content change.

• Archives of Pharmacal Research
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• 제17권3호
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• pp.139-144
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• 1994

A series of 6-(N-aylamono)-7-chloro-5, 8-quinolinedione derivatives was newly synthesized for the evaluation of antifugal activities. 5-Amino-8-hydroxy-quinoline (II) was treated with $KCLO_3$ in HCl to give 6,7-dichloro-5,8-quinolinediones (III). 6-(N-Arylamino)-7-chloro5,8-quinolinediones 1-13 were prepared by regioselective nucleophilic substitution of III with arylamines. In the presence of $CeCl_3$, the N-arylamono groups were introduced at the 6-position of 5,8-quinolinedione ring by the regioselective substitution. These derivatives 1-12 were tested for natifungal and also antibacterial activites, in vitro, against Canadida albicans, Aspergillus nier, Tricophyton mentagrophytes, Bacillus subtilis, Pseudomonas aeruginosa, Staphylococcus aureus and Escherichia coil. The MIC values were determined by the two-fold agar/steak dilution method. Newly obtained 6-(N-arylamino)-7-chloro5,8-quinolinedione derivatives showed potent antifungal and antibacterial activities. Among these derivatives, 1,3,5,7,8 and 9 showed more potent antifungal activities than fluconazole and griseofulvin. Also most of derivatives were found to be more active than ampicillin against gram-positive bacteria. 1 and 7 showed the very potent antifungal activities. 1 was the most efective in preventing the growth of Candida albicans, Aspergillus niger, Tricophyton mentagrophytes, Bacillus subtills and Staphylococcus aureus at MIC $1.6\;\mu{g/ml}$.

• Archives of Pharmacal Research
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• 제28권2호
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• pp.216-219
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• 2005

Wogonin (5,7-dihydroxy-8-methoxyflavone) has been reported to exhibit a variety of biological properties including anti-inflammatory and neuroprotective functions. In this study, biological activities of diverse synthetic wogonin derivatives have been evaluated in two experimental cell culture models. Inhibitory activities of wogonin derivatives on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in BV2 microglial cells and on hydrogen peroxide ($H_{2}O_2$)-induced neuronal cell death in SH-SY5Y human neuroblastoma were examined. Wogonin derivatives such as WS2 and WS3 showed more potent suppressive activities on LPS-induced NO production and $H_{2}O_2$-induced cytotoxicity than wogonin itself. In addition, thiol substitution played a minor role in enhancing the activities of the derivatives. These findings may contribute to the development of novel anti-inflammatory and neuroprotective agents derived from wogonin.

• 대한화학회지
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• 제54권2호
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• pp.234-239
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• 2010

경유 첨가제로 사용할 수 있는 카보네이트 유도체를 합성하고 그들의 DCN 향상 효과를 살펴보았다. 1,2-글리세롤 카보네이트와 긴 알킬그룹을 가지는 지방산을 반응시켜 경유와 구조적으로 유사한 화합물을 얻었다. 경유에 대한 용해도를 증가시키기 위해 긴 체인 중간에 이중 결합을 도입하거나 카보닐 그룹의 알파 위치에 알킬기를 도입하였다. ASTM 방법을 통하여 측정한 이들의 DCN 증가 정도는 ~1 정도였으며 이 결과는 카보네이트 유도체 화합물이 연료 첨가제로서 사용이 가능하다는 것을 보여주고 있다.

• Archives of Pharmacal Research
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• 제9권2호
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• pp.75-79
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• 1986

The effect of phenothiazine derivatives on the thermotropic transition of liposomal lipid bilayer made of dipalmitoyl phosphatidylchline and dipalmitoyl phosphatidic acid was investigated with differential scanning calorimetry. The thermograms of the liposomal bilayer incorporated with levomepromazine, chlopromazine, prochloperazine, perphenazine and fluphenazine were obtained and the size of cooperative unit of the transition were calculated from the ratio of the van't Hoff enthalpy change to the calculated enthalpy change of the transition. The results showed that incorporation of phenothiazine derivatives into the liposomal bilayer reduced the transition temperature at which the transition from solid state to liquid-crystalline state occurs, and broadened the thermogram peaks. Phenothiazine derivatives also significantly reduced the size of cooperative unit of the transition. The effect of the drugs was proportional to the concentration of the drug in the bilayer. This means that phenothiazine derivatives might have significant fluidizing effects on the biomembrane. The sizes of cooperative unit were successfully corrlated with phar-macological activities of the drugs and the surface pressure increases of lipid monolayer by these drugs. These correlations might be ascribed to a possible hydrophobic nature of interaction between the biomembrane and the drugs involved in their pharmacology.

• Archives of Pharmacal Research
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• 제20권6호
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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.

• 문화기술의 융합
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• 제4권4호
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• pp.343-348
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• 2018

안토시아닌 유도체는 다수의 식물에서 적색, 보라색 및 청색을 나타내는 천연 화합물의 중요한 성분이다. 안토시아닌 분자는 2-페닐 벤조피릴리움 염의 폴리메톡시 유도체이다. 안토시아닌의 유익한 특성에도 불구하고 다양한 질병을 예방하거나 치료하는 효과는 생체 이용률에 달려 있다. 따라서 이 연구에서는 안토시안 유도체의 전기적 특성을 알아보기 위해 HyperChem8.0의 PM3 방법을 이용하여 안토시아닌 유도체의 총 에너지, 밴드갭, 정전포텐셜, 알짜 전하량을 계산하여 유도체의 전기화학적 특성을 조사 하였다.

• Current Applied Physics
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• 제18권12호
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• pp.1507-1512
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• 2018

The development of an organic-based aqueous redox flow battery (RFB) using quinone as an electroactive material has attracted great attention recently. This is because this battery is inexpensive, produces high energy density, and is environment friendly in stationary electrical energy storage applications. Herein, we investigate the redox potentials and solubilities of indole-5,6-quinone and indole-4,7-quinone derivatives in terms of the substituent effects of functional groups using theoretical calculations. Our results indicate that full-site substituted derivatives of indolequinone are more useful as active materials compared to single-site substituted derivatives. In particular, our calculations reveal that the substitution of $-PO_3H_2$ and $-SO_3H$ functional groups with multiple polar bonds is very effective in increasing the activity of the aqueous RFB. As a strategy to overcome the limitation that the aqueous solubility is intrinsically low because they are organic molecules, we suggest the substitution of functional groups with multiple polar bonds to the backbones of active organic materials. Among 180 indolequinone derivatives, 17 candidates that meet the redox potential standards ($${\leq_-}0.2V$$ or $${\geq_-}0.9V$$) and eight candidates with solubility exceeding 2 mol/L are identified. Three indolequinone derivatives that satisfy both conditions are finally presented as promising electroactive candidates for an aqueous RFB.

• 한국응용과학기술학회지
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• 제36권1호
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• pp.348-354
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• 2019

Dipalmitoyl phosphatidyl choline(DPPC), Polyphenol 유도체, 그리고 Hematoxylin-Eosin은 5분 동안 산성 상태에서 직접 초음파 처리하여 명확한 표준용액을 제공했다. $25^{\circ}C$에서 DPPC 계의 레시틴소포에서 폴리페놀유도체의 흡수특성은 흡수분광학에 의해 분석하였다. 레시틴소포에서 단량체와 이량체 사이의 폴리페놀유도체의 평형은 폴리페놀유도체의 저농도에서 존재했지만 올리고머는 레시틴소포의 고농도에서 소포안에 형성되었다. 폴리페놀유도체의 일정한 농도에 Bacteriorhodopsin(BR)을 첨가함으로써 DPPC의 상전이동안 폴리페놀유도체의 흡수비율(${\alpha}/{\beta}$)이 감소되었다. 기둥이 있는 곳에 라멜라 소포와 uni- and multilamella 응집체의 혼합물이 존재한다. 용출된 기둥과 혼합물사이의 속도 차이가 관찰되었으므로 기둥 용출된 라멜라반응 보다 촉매 효과를 나타냈다. DPPC 및 폴리페놀유도체에 대한 가수분해의 상전이 온도는 DPPC 및 폴리페놀유도체 보다 높게 측정되었다.

• Molecular & Cellular Toxicology
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• 제1권3호
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• pp.179-188
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• 2005

To develop the novel anti-allergic drug, many sophoricoside derivatives were synthesized. Among these derivatives, JSH-II-3, VI-3, VII-3, VIII-3, VII-20 and VII-20 (sodium salt) were selected and subjected to high throughput toxicity screening (HTTS) because they revealed strong IL-5 inhibitory activity and limitation of quantity. Single cell gel electrophoresis (Comet) assay, mouse lymphoma thymidine kinase ($tk^{+/-}$) gene assay (MOLY), chromosomal aberration assay in mammalian cells and Ames reverse mutation assay in bacterial system were used as simplified, inexpensive, short-term in vitro screening tests in our laboratory. Through the primary screening using the comet assay, we could choose the first candidates of sophoricoside derivatives with no genotoxic potentials as JSH-VI-3, VII-3, VII-20 and VII-20 (sodium salt). Also JSH-VII-3, VII-20 and VII-20 (sodium salt) are non-mutagenic in MOLY assay, while JSH-II-3 is mutagenic at high concentration with the presence of metabolic activation system in both comet assay and MOLY assay. The selected derivatives (JSH-VI-3, VII-3, VII-20 and VII-20 (sodium salt) are not mutagenic in S. typhimurium TA98 and TA100 strains both in the presence and absence of metabolic activation. From results of chromosomal aberration assay, 6 h treatment of JSH-VI-3, VII-3 and VII-20 (sodium salt) were not revealed clastogenicity both in the presence and absence of S-9 mixture. Therefore, we suggests that JSH-VI-3, VII-3, VII-20 and VII-20 (sodium salt), as the optimal candidates with both no genotoxic potential and IL-5 inhibitory effects must be chosen. To process the development into new anti-inflammatory drug of these derivatives, further investigation will need.