• Archives of Pharmacal Research
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• 제24권1호
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• pp.27-34
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• 2001

A series of 2-methylbenzimidazole incorporated to different heterocycles through ethyl or carbamoylethyl groups at position 1 of benzimidazole were synthesized. Also 3-(2-methylbenzimidazol-1-yl)propanoic acid hydrazide incorporated with semicarbazides and thiosemicarbazides were prepared. Moreover, the triazole 5e underwent Michael addition and alkylation reaction. Some of the newly synthesized compounds showed considerable antimicrobial activity against gram positive, negative bacteria and yeast.

• Bulletin of the Korean Chemical Society
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• 제30권9호
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• pp.1933-1938
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• 2009

New $\pi$-conjugated polymer with vinylene linkage, poly((10-hexyl-3,7-phenothiazine)-alt-(4-(4-butyl-phenyl)- 3,5-diphenyl-4H-[1,2,4]triazole)-3,5-vinylene) (PTV-TAZ) was synthesized by the Heck coupling reaction. The photoluminescence (PL) maximum wavelength and the band gap energy of PTV-TAZ film were 555 nm and 2.41 eV, respectively. The HOMO energy level of PTV-TAZ was -4.99 eV, which was slightly lower than that of PTV (-4.89 eV). Electron deficient aromatic 1,2,4-triazole (TAZ) in the polymer backbone does not affect the HOMO energy level significantly. The maximum efficiency and brightness of double layer structured electroluminescent (EL) device (ITO/PEDOT (30 nm)/PTV-TAZ (60 nm)/Al) were 0.247 cd/A and 553 cd/$m^2$, respectively, which were significantly higher than those of the device based PTV (1.65 ${\times}\;10^{-4}$ cd/A and 4.3 cd/$m^2$). This is due to that TAZ unit improves electron transporting ability in the emissive layer. The turn-on voltage (defined as the voltage required to give a luminescence of 1 cd/$m^2$) of brightness of the device based on PTV-TAZ was 12.0 V, which was similar to that the based on PTV (11.5 V). This is due to that the ionization potential of PTV-TAZ is very similar to that of PTV.

• 원예과학기술지
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• 제18권6호
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• pp.823-826
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• 2000

본 실험은 왜화제인 daminozide, chlormequat, hexaconazole, uniconazole, paclobutrazole과 triazole계 살균제인 diniconazole, myclobutanil, difenoconazole, tebuconazole, bitertanol 등이 'New Guinea' 임파첸스의 삽수발근에 미치는 영향을 조사하기 위하여 수행하였다. 왜화제 처리에 의한 부정근의 형성은 'Papete'와 'Anguilla'에서 daminozide를 제외한 모든 약제에서 촉진되었으며 hexaconazole, uniconazole과 paclobutrazole 처리에서 chlormequat보다 더 많은 부정근이 형성되었다. 최장근의 길이와 근권은 'Papete'에서 chlormequat, hexaconazole, uniconazole 및 pac1obutrazol의 비교적 높은 농도에서 감소되었으나 'Anguilla' 품종에서는 차이가 적었다. 한편, triazole계 살균제처리에 의한 부정근의 형성은 'Papete'와 'Martinique' 품종에서 현저하게 촉진되었으며 'Pagopago'에서는 큰 영향이 없었다. 최장근의 길이와 근권은 'Martinique'와 'Pagopago'에서 'Papete'에 비하여 민감한 반응을 보였다. 이와 같은 결과들은 발근촉진을 위하여 triazole계 살균제들이 효과적으로 사용될 수 있다는 것을 제시한다.

• 한국추진공학회지
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• 제20권6호
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• pp.11-17
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• 2016

BTTN, TMETN은 고체 추진제에서 사용되는 대표적인 에너지 가소제이다. 그러나 이 물질들은 충격 감도가 비교적 민감하다는 단점이 있다. 본 연구에서는 BTTN, TMETN 보다 둔감한 에너지 가소제를 개발하기 위해 트리아졸 계열의 4,5-bis(azidomethyl)-(2-methoxyethyl)-1,2,3-triazole(DAMETR)을 합성하고 이화학적 특성 분석을 하였다. 또한, 분광분석(NMR, IR)을 통해 DAMETR의 구조를 분석하였고, 유리전이온도, 녹는점, 분해온도, 밀도, 점도, 충격감도 등의 물리적 특성을 측정하였다. 그리고 Gaussian 09와 EXPLO5를 이용하여 생성열과 폭발 특성(폭압, 폭속) 등을 계산하였다. 특히 1-DAMETR(>50 J)의 충격감도는 BTTN(1 J), TMETN(9.2 J)에 비해 매우 둔감하였다.

• 한국추진공학회지
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• 제21권6호
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• pp.32-38
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• 2017

가소제는 추진제 혼화 시 흐름성과 공정성을 향상시키는 역할을 한다. 대표적인 가소제로서 DOS, DOA, IDP, BTTN 등이 있다. 특히 BTTN은 에너지 가소제로서 추진제 성능에 도움을 주는 물질이며, 다양하게 사용되고 있다. 그러나 이 물질들은 충격감도가 비교적 민감하다는 단점이 있다. 본 연구에서는 둔감한 에너지 가소제를 개발하기 위해 트리아졸 계열의 4,5-bis (azidomethyl)-(1-butyl)-1,2,3-triazole (1-DABTR)을 합성하고 이화학적 특성 분석을 하였다. 또한, 분광분석(NMR, IR)을 통해 1-DABTR의 구조를 분석하였고, 유리전이온도, 녹는점, 분해온도, 밀도, 점도, 충격감도 등의 물리적 특성을 측정하였다. 그리고 Gaussian 09를 이용하여 생성열을 계산하였다.

• 대한화학회지
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• 제60권2호
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• pp.125-130
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• 2016

With the goal of developing Alzheimer’s disease therapeutics, we have designed and synthesized new triazole linked decursinol derivatives having potency inhibitory activities against cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)]. Since inhibition of cholinesterase (ChE) is still considered to be one of the most effective targets to treat AD patients, many new classes of ChE inhibitors have been synthesized. In an effort of identifying new type of cholinergic drug, decursinol derivatives 11-17 have been synthesized between decursinol and other biological interesting compounds such as lipoic acid, polyphenols, etc by using the click reaction and then evaluated their biological activities. Compound 12 (IC₅₀ = 5.89 ± 0.31 mM against BuChE) showed more effective inhibitory activity against BuChE than galantamine (IC₅₀ = 9.4 ± 2.5 mM). Decursinol derivatives can be considered a new class inhibitor for BuChE and can be applied to be a novel drug candidate to treat AD patients.

• 한국대기환경학회지
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• 제21권6호
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• pp.593-603
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• 2005

Passive sampler using 4-amino-3-hydrazino-5-mercapto-1, 2, 4-triazole (AHMT) was developed to determine formaldehyde in indoor environment. The chromatography paper cleaned by $3\%$ hydrogen peroxide solution was experimently determined as a optimum absorbtion filter for the collection of formaldehyde. The passive sampler with a broad cross-sectional area and a short diffusion length was quite good in sensitivity. The passive sampler and the active sampling method with an impinger were strongly correlated with a correlation coefficient of 0.9848. The limits of detection and quantification of the passive sampler for the measurement of formaldehyde in the indoor environment were 7.5 and 10.2 ppb, respectively. Temperature ($19\∼28^{circ}C$) and relative humidity ($30\∼90\%$) had slight influence on the sampling rate of the passive sampler. However, the increase of flow velocity on the surface of sampler resulted in the increase of sampling rate.

• 한국응용과학기술학회지
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• 제24권2호
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• pp.109-116
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• 2007

2-Chlorobenzoyl hydrazine refluxed with benzoyl isothiocyanate and phenyl isothiocyanate in ethanol for 3 hours to give benzamide derivative (1) and anilinederivative (2) on yield of 71%and 95%, respectively. Benzamide derivative (1) reacted with ethanolic sodium hydroxide on reflux to afford cyclization product (3), followed by general substitution reaction of two steps to give acetamide (5), and derivatived acetamides 7a-7k, while aniline derivative (2) reacted with ethanolic sodium hydroxide on reflux to afford another cyclization product (4). Thiol (4) reacted with N-phenyl chloroacetamide in the presence of potassim carbonate to give acetamide derivative (6). Compounds 1-7kwere evaluated for their growth inhibition against five cancer cell lines, including human lung carcinoma (A-549), human prostate cancer (DU145), human colon adenocarcinoma (HT-29), human malignant melanoma (SK-MEL-2) and human ovary malignant ascites (SK-OV-3) with sulforhodamine B (SRB) assay. All compounds (1-7k) showed low inhibition activities under 50% on 100M concentration.

• Mass Spectrometry Letters
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• 제9권2호
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• pp.61-65
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• 2018

KPLA-012, a benzopyranyl 1,2,3-triazole compound, is considered a potent $HIF-1{\alpha}$ inhibitor based on the chemical library screening, and is known to exhibit anti-angiogenetic and anti-tumor progressive effects. The aim of this study was to investigate the pharmacokinetic properties of KPLA-012 in ICR mice and to investigate in vitro characteristics including the intestinal absorption, distribution, metabolism, and excretion of KPLA-012. The oral bioavailability of KPLA-012 was 33.3% in mice. The pharmacokinetics of KPLA-012 changed in a metabolism-dependent manner, which was evident by the low recovery of parent KPLA-012 from urine and feces and metabolic instability in the liver microsomes. However, KPLA-012 exhibited moderate permeability in Caco-2 cells ($3.1{\times}10^{-6}cm/s$) and the metabolic stability increased in humans compared to that in mice (% remaining after 1 h; 47.4% in humans vs 14.8% in mice). Overall, the results suggest that KPLA-012 might have more effective pharmacokinetic properties in humans than in mice although further studies on its metabolism are necessary.

• Journal of Microbiology and Biotechnology
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• 제14권4호
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• pp.693-697
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• 2004

YH-1715R, (2R,3R)-2-(2,4-difluorophenyl)-3-(3-methoxy-1,2,4-isothiazol-3-yl-thio)-1-( 1H-1,2,4-triazol-l-yl)-2-butanol, a new triazole derivative obtained by the structural modification of fluconazole, was found to exhibit potent anti-Candida activity against a wide variety of Candida albicans (C. albicans) (MIC: 0.4-12.5 mg/l). To investigate the mode of action of YH-1715R, its effect on ergosterol biosynthesis in cell-free extracts and whole cells of C. albicans was examined. The inhibitory activity of YH-1715R was approximately ten-fold higher than that of fluconazole. To determine the primary action mechanism of YH-1715R, its inhibitory activity against lanosterol $14\alpha$-demethylase (14$\alpha$-DM), a major target for azole, was measured using gas-liquid chromatography. YH-1715R and fluconazole were found to inhibit 14a-DM with an $IC_{50}$ of 0.015 $\mu$M and 0.01$8\mu$M, respectively, plus the mode of inhibition of YH-1715R and fluconozole was noncompetitive with a $K_i$ of 0.0533$\mu$M and 0.0975$\mu$M.