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Lee Jiseong,Parmbil Saranya Kattil,Pandit Nagendar Kumar,Kumar Sunil,Syed Asad,Elgorban Abdallah M.,Wong Ling Shing,Ranjana,Kim Hoon,Mathew Bijo 한국응용생명화학회 2024 Applied Biological Chemistry (Appl Biol Chem) Vol.67 No.-
Nine morpholine-derived halogenated chalcone derivatives (MHC1-MHC9) were synthesized, and their inhibitory activity against monoamine oxidase (MAO) was evaluated. MHC5 showed the highest inhibitory activity against MAO-B with an IC50 value of 0.065 μM, followed by MHC7 (IC50=0.078 μM) and MHC6 (IC50=0.082 μM). The para-F substituent MHC4 was also potent (IC50=0.095 μM). The selectivity index values of all the compounds were high for MAO-B over MAO-A, and the values for MHC5 and MHC4 were 66.15 and 80.11, respectively. MHC5 and MHC4 were competitive MAO-B inhibitors with Ki values of 0.024±0.00062 and 0.041±0.0028 μM, respectively. In reversibility tests, the changes in residual activity before and after the dialysis of MHC5 and MHC4 were similar to those of safnamide, a reversible MAO-B reference inhibitor. Additionally, molecular docking and dynamic simulations predicted that the lead molecules MHC5 and MHC4 could strongly bind to the MAO-B active site with docking scores of –10.92±0.08 and –10.64±0.14 kcal/mol, respectively. Additionally, MHC4 and MHC5 exhibited favorable ADME features, including blood–brain barrier permeability. The experiments confrmed that MHC5 and MHC4 are reversible and potent selective inhibitors of MAO-B and are promising candidates for the treatment of neurodegenerative diseases (human health).
Chitosan 첨가와 template 종류에 따른 SAPO-34 촉매 특성 분석 및 DTO 반응 연구
윤영찬,최기환,김효섭,이동희,박주식,김영호 한국공업화학회 2015 한국공업화학회 연구논문 초록집 Vol.2015 No.1
DME(dimethyl ether)는 천연가스나 석탄 또는 바이오매스 등의 다양한 에너지원으로부터 제조할 수 있을 뿐만 아니라 연소시 오염물질의 발생량이 적은 친환경적 연료중의 하나로 주목받고 있다. 현재 DME의 이용 기술로서 DME로부터 올레핀 제조(DTO ; DME to olefins)반응이 촉매 개발과 함께 많은 연구가 진행되어 오고 있다. DTO 반응의 전형적인 촉매로서 SAPO-34는 경질 올레핀 선택도가 매우 높은 촉매로 알려져 있다. 본 연구에서 메조세공을 가지는 SAPO-34 촉매를 제조하기 위해 mesopore-generating agent로 chitosan을 사용하였고 template 종류가 SAPO-34 촉매에 미치는 영향을 알아보기 위해 morpholine과 TEAOH를 template로 사용하여 수열합성법을 통해 제조하였다. 제조된 SAPO-34 분자체는 Scanning electron microscopy(SEM)와 temperature-programmed NH<sub>3</sub> desorption을 사용하여 특성 분석하였다.
정병호,조원제,천승훈,박면지,유진철,천문우 朝鮮大學校 1998 藥學硏究誌 Vol.19 No.2
For the development of antifungal agents. modification of naftifine which exhibits significant antimycotic activity was performed by replacing the naphthalene ring of it to hetero cyclic rings such as morpholine. benzothiazole. piperidine and pyridine derivatives. The synthesized compounds were tested in vitro antifungal activity against five different fungi with naftifine as a comparative antimycotic molecule. From the biological evaluation two compounds. (E)-N-(3-phenyl-2-propenyl)-N-(4-piperidinylmethyl)amine(3d) and (E)-N-(3-phenyl-2-propenyl)-N-(3-pyndylmethyl)amine(3D) showed relatively noticeable activity(MIC=50㎍/㎖). On the other hand. the other compounds had no activity.
정병호(Byung Ho Chung),조원제(Won Jea Cho),천승훈(Seung Hoon Cheon),박면지(Myun Ji Park),유진철(Jin Cheol Yoo),천문우(Moon Woo Chun) 대한약학회 1997 약학회지 Vol.41 No.2
For the development of antifungal agents, modification of naftifine which exhibits significant antimycotic activity was performed by replacing the naphthalene ring of it to hetero cyclic rings such as morpholine. benzothiazole, piperidine and pyridine derivatives. The synthesized compounds were tested in vitro antifungal activity against five different fungi with naftifine as a comparative antimycotic molecule. From the biological evaluation two compounds, (E)-N-(3-phenyl-2-propenyl)-N-(4-piperidinylmethyl)amine(3d) and (E)-N-(3-phenyl-2-propenyl)-N-(3-pyridylmethyl)amine(3f) showed relatively noticeable activity(MIC=50mcg/ml). On the other hand, the other compounds had no activity.
홍혜리,문권모,Thuy-Tien Thi Trinh,Tae-Hui Eom,박현,김학성,여선주 대한기생충학ㆍ열대의학회 2024 The Korean Journal of Parasitology Vol.62 No.1
Antimalarial drugs are an urgently need and crucial tool in the campaign against malaria,which can threaten public health. In this study, we examined the cytotoxicity of the 9 antimalarial compounds chemically synthesized using SKM13-2HCl. Except for SKM132HCl, the 5 newly synthesized compounds had a 50% cytotoxic concentration (CC50)>100 µM, indicating that they would be less cytotoxic than SKM13-2HCl. Among the 5compounds, only SAM13-2HCl outperformed SKM13-2HCl for antimalarial activity,showing a 3- and 1.3-fold greater selective index (SI) (CC50/IC50) than SKM13-2HCl in vitro against both chloroquine-sensitive (3D7) and chloroquine -resistant (K1) Plasmodiumfalciparum strains, respectively. Thus, the presence of morpholine amide may help to effectively suppress human-infectious P. falciparum parasites. However, the antimalarialactivity of SAM13-2HCl was inferior to that of the SKM13-2HCl template compound inthe P. berghei NK65-infected mouse model, possibly because SAM13-2HCl had a lowerpolarity and less efficient pharmacokinetics than SKM13-2HCl. SAM13-2HCl was moretoxic in the rodent model. Consequently, SAM13-2HCl containing morpholine was selected from screening a combination of pharmacologically significant structures as being the most effective in vitro against human-infectious P. falciparum but was less efficient in vivo in a P. berghei-infected animal model when compared with SKM13-2HCl. Therefore, SAM13-2HCl containing morpholine could be considered a promising compound to treat chloroquine-resistant P. falciparum infections, although further optimization is crucial to maintain antimalarial activity while reducing toxicity in animals.
Fengyan Ge,Chun Yang,Zaisheng Cai 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.11
A novel reactive fluorescent dye [2-morpholine-4-(6-chlorine-1,3,5-s-triazine)-amino]fluorescein based on 5-aminofluorescein was synthesized by electrophilic substitution. The photophysical properties, solvent effect, pH value sensitivity, and metal ions responsibility of this new fluorophore were investigated. Compared with 5-aminofluorescein, the novel fluorophore exhibited stronger fluorescence and longer lifetime. The fluorescence property of the new dye was obviously affected by different solvents and pH values, and it showed stronger fluorescence in the protic solvents or an alkaline environment. Moreover, the fluorescent intensity could be enhanced by the formation of complex with metal ions especially with Mg2+. The results show that the fluorescent dye is a promising efficient sensor for solvents, protons, and metal ions.
QuEChERS법과 LC-MS/MS를 이용한 농산물 중 Fenpropimorph 시험법 개발 및 검증
이한솔,도정아,박지수,조성민,신혜선,장동은,최영내,정용현,이강봉 한국식품위생안전성학회 2019 한국식품위생안전성학회지 Vol.34 No.2
An analytical method was developed for the determination of fenpropimorph, a morpholine fun- gicide, in hulled rice, potato, soybean, mandarin and green pepper using QuEChERS (Quick, Easy, Cheap, Effective, Rugged and Safe) sample preparation and LC-MS/MS (liquid chromatography-tandem mass spectrometry). The QuEChERS extraction was performed with acetonitrile followed by addition of anhydrous magnesium sulfate and sodium chloride. After centrifugation, d-SPE (dispersive solid phase extraction) cleanup was conducted using anhy- drous magnesium sulfate, primary secondary amine sorbents and graphitized carbon black. The matrix-matched cali- bration curves were constructed using seven concentration levels, from 0.0025 to 0.25 mg/kg, and their correlation coefficient (R2) of five agricultural products were higher than 0.9899. The limits of detection (LOD) and quantifica- tion (LOQ) were 0.001 and 0.0025 mg/kg, respectively, and the limits of quantification for the analytical method were 0.01 mg/kg. Average recoveries spiked at three levels (LOQ, LOQ×10, LOQ×50, n=5) and were in the range of 90.9~110.5% with associated relative standard deviation values less than 5.7%. As a result of the inter-laboratory val- idation, the average recoveries between the two laboratories were 88.6~101.4% and the coefficient of variation was also below 15%. All optimized results were satisfied the criteria ranges requested in the Codex guidelines and Food Safety Evaluation Department guidelines. This study could serve as a reference for safety management relative to fen- propimorph residues in imported and domestic agricultural products.