• Title/Summary/Keyword: Pyridyl-N

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Smile Rearrangement of Herbicidal Flazasulfuron (제초성 Flazasulfuron의 Smile 자리옮김 반응)

  • Lee, Gwnag-Jae;Kim, Yong-Jip;Kim, Dae-Whang;Sung, Nack-Do
    • Applied Biological Chemistry
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    • v.39 no.1
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    • pp.70-76
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    • 1996
  • A series of the herbicidal pyridylsulfonyl areas, none substitutent, 1-(4,6-dimethoxypyrimidine-2-yl)-3-(2-pyridylsulfonyl) urea, 3 and 3-trifluoromethyl substitutent, 1-(4,6-dimethoxypyrimidine-2-yl)-3-(3-trifluoromethyl-2-pyridylsulfonyl) urea, 5(Flazasulfuron) were synthesizied and the rate of hydrolysis of their has been studied in 25%(v/v) aqueous dioxane at $45^{\circ}C$. From the results of solvent effect($m{\ll}1,\;n{\ll}3\;&\;{\mid}m{\mid}{\ll}{\mid}{\ell}{\mid}$), thermodynamic parameter (${\Delta}S^{\neq}=0.54{\sim}\;-2.19\;e.u.\;&\;{\Delta}H^{\neq}=0.025\;Kcal.mol.^{-1}$), hydrolysis product analysis, $pK_a$ constant(3: 4.9 & 5: lit.4.6) and the rate equation, a marked difference in the kinetics of the reaction of 3 and 5(Flazasulfuron) was observed. It may be concluded that the hydrolysis of 5 proceeds through the $A-S_N2Ar$ reaction via conjugate acid$(5H^+)$ below pH 7.0, whereas, above pH 9.0, the hydrolysis proceeds through irreversibly $(E_1)_{anion}$ and reversibly $(E_1CB)_R$ mechanism via conjugate base(CB), respectively. But in case of 5, $A-S_N2Ar,\;(E_1)anion\;and\;(E_1CB)_R$ mechanism involved Smile rearrangement. The mate of rearrangement of 5 to a 3-trifluoromethyl-2-pyridylpyrimidinyl urea(PPU) in acid and 3-trifluoromethyl-2-pyridyl-4.6-dimethoxypyridinyl amine (PPA) in base was increased about 3.5 times by the introduction of trifluoromethyl group in the 3-position on the 2-pyridyl ring. From the basis of these findings, a possible mechanism for the hydrolysis of 5 was proposed and discussed.

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4-(N-Methyl-N-nitrosamino)-1(3-pyridyl)-1-butanone(NNK) Restored the Cap-dependent Protein Translation Blocked by Rapamycin

  • Kim Jun-Sung;Park Jin Hong;Park Sung-Jin;Kim Hyun Woo;Hua Jin;Cho Hyun Sun;Hwang Soon Kyung;Chang Seung Hee;Tehrani Arash Minai;Cho Myung Haing
    • Toxicological Research
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    • v.21 no.4
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    • pp.347-353
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    • 2005
  • Eukaryotic initiation factor 4E (elF4E) is a key element for cap-dependent protein translation controlled by affinity between elF4E and 4E-binding protein 1 (4E-BP1). Rapamycin can also affect protein translation by regulating 4E-BP1 phosphorylation. Tobacco-specific nitrosamine, 4(N-methyl-N-nitrosamino )-1-(3-pyridyl)-1-butanone (NNK) is a strong lung carcinogen, but its precise lung cancer induction mechanism remains unknown. Relative roles of cap-dependent and -independent protein translation in terms of NNK-induced lung carcinogenesis were elucidated using normal human bronchial epithelial cells. NNK concentrations applied in this study did not decrease cell viability. Addition of NNK restored rapamycin-induced decrease of protein synthesis and rapamycin-induced phosphorylation of 4E-BP1, and increased expression levels of mTOR, ERK1/2, p70S6K, and Raf-1 in a concentration-dependent manner. NNK also caused perturbation of normal cell cycle progression. Taken together, NNK might cause toxicity through the combination of restoration of 4E-BP1 phosphorylation and increase of elF4E as well as mTOR protein expression, interruption of Raf1/ERK as well as the cyclin G-associated p53 network. Our data could be applied towards elucidation of the molecular basis for lung cancer treatment.

Comparison of in vitro propagation and occurrence of morphological and genetic variation in strawberry tissue culture with various plant hormone treatments (딸기 조직배양 시 여러가지 식물호르몬 처리에 따른 기내 증식 및 형태적, 유전적 변이 발생 비교)

  • Kim, Hye Jin;Lee, Jong Nam;Choi, Mi Ja;Suh, Jong Taek
    • Journal of Plant Biotechnology
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    • v.46 no.2
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    • pp.106-113
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    • 2019
  • The objective of this study was to carry out treatment of various plant hormones in order to determine morphological and genetic variation degree of tissue-cultured strawberry. The cultivar used in this experiment was 'Goha' and 'Seolhyang', the plant hormones used for experiment were benzyladenine (BA), N-(2-Chloro-4 pyridyl)-N'-phenylurea (CPPU) and thidiazuron (TDZ), and the concentrations were 0.5, 1.0, 2.0, $4.0mg{\cdot}L^{-1}$ with each hormone. The BA treatment of the proliferation efficiency of tissue-cultured strawberry 'Goha' and 'Seolhyang' was the highest. When processing BA, CPPU and TDZ, morphological variation and genetic variation happened in strawberry 'Goha' and 'Seolhyang', especially, the variations appeared highly in CPPU treatment. The genetic variation in 'Goha' appeared at the concentration more than BA $0.5mg{\cdot}L^{-1}$ as 1.1%, appeared at the concentration of CPPU $0.5mg{\cdot}L^{-1}$ as 15.3%, and at the concentration of TDZ $2.0mg{\cdot}L^{-1}$ as 1.2%. The genetic variation in 'Seolhyang' appeared at the concentration of BA $4.0mg{\cdot}L^{-1}$ as 2.3%, and at the concentration of CPPU $0.5mg{\cdot}L^{-1}$ as 14.3%. Therefore, CPPU should not be treated during strawberry tissue culture, and BA and TDZ should be treated at low concentration.

Interaction of a Pyridyl-Terminated Carbosiloxane Dendrimer with Metal Ions at the Air-Water Interface

  • Lee, Burm-Jong;Kim, Seong-Hoon;Kim, Chung-kyun;Shin, Hoon-Kyu;Kwon, Young-Soo
    • KIEE International Transactions on Electrophysics and Applications
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    • v.3C no.6
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    • pp.216-219
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    • 2003
  • A new class of carbosiloxane dendrimer (G4-48PyP) terminated with 4-pyridylpropano I was synthesized and its possible application to functional thin films was examined through metal complexation and Langmuir-Blodgett (LB) technique. The highly concentrated periphery pyridyl groups of G4-48PyP were exposed on aq. aluminum ions at the air-water interface. The monolayers showed stability up to ca. 50 mN/m of surface pressure. When the subphase became acidic or alkaline, the monolayers changed to condensed phase. The presence of aluminum ions also caused reduction of the molecular area. The macroscopic images of the monolayers were monitored by Brewster angle microscopy (BAM) and only the images of dendrimer aggregates could be observed after the monolayer collapse. The surface images of the monolayer LB film were scanned by atomic force microscopy (AFM). The convex structures of single and aggregate molecules were directly observed. The structures of Langmuir-Blodgett (LB) films were characterized by FT-IR, UV-Vis, and X-ray photoelectron spectroscopy (XPS). The UV-Vis spectrum of the aluminum ion-complexed LB film showed additional band around 670nm, which was not found in the spectra of dendrimer itself or aq. aluminum ions. XPS spectra also supported the incorporation of aluminum ions into the LB films.

Detection of ClO4- via A Hypersensitive Receptor : Unusual Electrostatic Equilibria between Host and Guest in Aqueous Media (고감도 수용체에 의한 ClO4- 검출 : 수용액에서 주-객 이온간의 평형)

  • Lee, Young-A;Hong, Jongki;Jung, Ok-Sang
    • Analytical Science and Technology
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    • v.15 no.1
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    • pp.31-35
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    • 2002
  • A useful receptor for the sensing of ${CIO_4}^-$ species with remarkable selectivity has been developed. The hypersensitive interaction between a host and a guest has been investigated for the complex $[Pd(Me_4en)(Py_2S){\cdot}2ClO_4]_4$ ($Me_4en$ = N,N,N',N'-tetramethylethylenediamine; $Py_2S$ = 4,4'-dipyridyl sulfide). The pyridyl moiety of $Py_2S$ exhibits two sets of $^1H$ resonances that are delicately dependent upon temperature, concentration, and media. The nonrigidity has been explained in terms of an electrostatic equilibrium between the tetrameric host and the ${CIO_4}^-$ guest. The equilibrium is a useful method for the detection of ${CIO_4}^-$ anion with remarkable selectivity via "a restricted guest within a big host" in aqueous solution.

Effect of Cationic and Anionic Porphyrins on the Structure and Activity of Adenosine Deaminase

  • Ajloo, Davood;Hajipour, Samaneh;Saboury, Ali Akbar;Zakavi, Saeed
    • Bulletin of the Korean Chemical Society
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    • v.32 no.9
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    • pp.3411-3420
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    • 2011
  • Kinetic and structural studies have been carried out on the effects of meso-tetrakis(4-sulfonatophenyl)-porphyrin ($H_2TPPS_4$) as an anionic and meso-tetrakis(3-N-methyl-pyridyl)porphyrin ($H_2TMPYP$) as a cationic porphyrin with adenosine deaminase (ADA) in 25 mM citrate/phosphate buffer, pH = 4-8, at $37^{\circ}C$ using UVvis spectrophotometry, circular dichroism (CD), fluorescence spectrophotometry as well as molecular dynamics (MD) and molecular docking. Kinetic results showed that the two porphyrins are non-competitive inhibitors. Increasing pH, increases $K_I$ and cationic porphyrin has a higher $K_I$ and lower binding constant ($K_b$) at all pH ranges. Analyzing the secondary structure revealed that both ligands decrease the secondary structure and that the anionic porphyrin is more effective.

Receptor-Ligand Binding Characteristics of KR-31064 (KR-31064의 수용체-리간드 결합특성에 대한 연구)

  • Lee, Sunghou
    • YAKHAK HOEJI
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    • v.58 no.1
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    • pp.16-20
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    • 2014
  • KR-31064 was developed for the strong angiotensin II receptor antagonist among the one of pyridyl imidazol series compounds. To investigate the receptor-ligand binding characteristics of this nonpeptide antagonist, binding experiments were deployed in various conditions and ex vivo contractile responses were tested toward the standard compound, losartan. Receptor binding experiments with radiolabeled angiotensin II, the $IC_{50}$ value for KR-31064 resulted 0.67 nM without any activities toward type 2 angiotensin II receptor. The comparative potency against losartan was more than 18 fold and the specific activity in type 1 angiotensin II receptor was more than 10,000 fold comparing to the type 2 receptor. Scatchard analysis of saturation binding data showed KR-31064 acted on the receptor in a competitive mode. KR-31064 inhibited the contractile response derived by angiotensin II ($pK_B$: 9.86) similar to that of losartan with decreased maximum signals. As a potent and specific type 1 angiotensin II receptor antagonist, KR-31064 may have possibilities for the development of diagnostic ligands that can be used as tools for various biochemical research experiments and non-invasive diagnostics.

Synthesis, Characterizations, and Intramolecular Quenching Behavior of an Axially-Linked Trinuclear Molecular Wire Containing Ruthenium(II) Porphycenes

  • Abe, Masaaki;Ashigara, Shiho;Okawara, Toru;Hisaeda, Yoshio
    • Rapid Communication in Photoscience
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    • v.4 no.1
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    • pp.22-24
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    • 2015
  • A new trinuclear complex $[Ru(TPrPc)(CO)]_2[Ru(pytpy)_2](PF_6)_2$ (TPrPc = 2,7,12,17-tetra-n-propylporphycenato dianion and pytpy = 4'-(4-pyridyl)-2,2':6',2"-terpyridine) has been synthesized and characterized as the first example of a discrete molecular wire containing metalloporohycenes as a building block. The trinuclear complex shows multiple-step redox behavior in 0.1 M n-$Bu_4NPF_6$-dichloromethane. The mononuclear $[Ru(pytpy)_2]^{2+}$ precursor shows emission at 640 nm (deaerated acetone, 298 K) upon illumination at the metal-to-ligand charge transfer (MLCT) band at 495 nm, but the trinuclear molecular wire is found to be non-emissive upon photoexcitation at the central $[Ru(pytpy)_2]^{2+}$ entity, indicating an efficient quenching ability of the axially-linked, ruthenium(II)-porphycene chromophores in an intramolecular fashion.

A Hybrid Spacer Effect on White Organic Light-Emitting Diodes with Phosphorescent Emitters (인광 발광 물질을 이용한 백색 유기 발광 다이오드에서의 혼합된 스페이서의 영향에 관한 연구)

  • Seo, Ji-Hoon;Park, Jung-Sun;Hyung, Gun-Woo;Seo, Ji-Hyun;Lee, Kum-Hee;Yoon, Seung-Soo;Kim, Young-Kwan
    • Journal of the Korean Applied Science and Technology
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    • v.26 no.1
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    • pp.24-28
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    • 2009
  • 본 논문에서는 청색 인광 발광 물질인 bis(3,5-Difluoro-2-(2-pyridyl)phenyl-(2-carboxypyridyl) iridium (III) (Flrpic)과 녹색 인광 발광 물질인 fac-tris(2-phenypyridine) irdium(III) ($Ir(ppy)_3$)와 적색 인광 발광 물질인 his(5-benzoyl-2-phenylpyridinato-C,N)iridium(III) (acetylacetonate) ($(Bzppy)_{2}Ir(acac)$)를 각각 적층하여 백색 유기 발광 다이오드를 제작하였고, 각각의 발광층 사이에 혼합된 스페이서인 4,4'-N,N'-dicarbazole-biphenyl (CBP):4,7-diphenyl-1,10-phenanthroline (BPhen)을 적층하여 그 때의 영향에 대하여 연구하였다. 최적화된 구조에서의 전력 효율은 $0.014\;mA/cm^2$에서의 19.7 lm/w를 나타내었으며, $0.127\;mA/cm^2$에서의 11.5%의 외부 양자 효율을 나타내었고, 8 V에서 Commission Internationale do I'Eclairage ($CIE_{x,y}$) coordinates (x=0.36, y=0.44)의 색좌표를 나타내었다.

In vitro Antioxidant Activity of Ethanolic Extract of Chlorophytum borivilianum

  • Govindarajan, R.;Sreevidya, N.;Vijayakumar, M.;Thakur, M.;Dixit, V.K.;Mehrotra, S.;Pushpangadan, P.
    • Natural Product Sciences
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    • v.11 no.3
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    • pp.165-169
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    • 2005
  • Chlorophytum borivilianum Baker (Antharicaceae) commonly referred as 'Safed Musli' has been widely used in the Indian traditional systems of medicine to treat various diseases like rheumatism apart from having immunomodulating property and is used as general tonic. It is also known as 'Ayurvedic viagra' for its aphordisiac properties. C. borivilianum was screened for the first time to determine its antioxidant activity, isolation of the sapogenins and standardization of the isolated sapogenin fraction using HPTLC. Potent antioxidant activity of ethanolic extract was found by their ability to scavenge DPPH (84.51%), hydroxyl radical (48.95 %), ferryl bi-pyridyl complex (84.53%) along with the inhibition of lipid peroxidation (67.17%) at $100\;{\mu}g/ml$ concentration. The ethanolic extract also exhibited significant inhibition of superoxide anion radical generated by photochemiluminescence. Thus, the potent antioxidant activity validates the innumerable therapeutic claims of the plant in the traditional system especially its use as a Rasayana drug.