• 제목/요약/키워드: 2-a]pyrimidine

검색결과 167건 처리시간 0.022초

A Convenient Synthesis of New 3,7-Diphenylthieno[3,2-e]bis[1,2,4] triazolo[4,3-a:4',3'-c]pyrimidine Derivatives by Oxidative Cyclization Using Alumina-supported Calcium Hypochlorite

  • Son, Hoon-Young;Song, Yang-Heon
    • Bulletin of the Korean Chemical Society
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    • 제31권8호
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    • pp.2242-2246
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    • 2010
  • New 3,7-diphenylthieno[3,2-e]bis[1,2,4]triazolo[4,3-a:4',3'-c]pyrimidine derivatives were easily synthesized at room temperature in good yield by the oxidative cyclization of thienopyrimidinyl hydrazones with alumina-supported calcium hypochlorite ($Ca(OCl)_2/Al_2O_3$).

Synthesis and Antimicrobial Screening of Pyrimidine Annulated Dihydropyrano[2, 3-c]pyrazole Derivatives

  • Hegde, Hemant;Ahn, Chuljin;Waribam, Preeti;Shetty, Nitinkumar S.
    • 대한화학회지
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    • 제62권2호
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    • pp.87-92
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    • 2018
  • A series of pyrimidine annulated dihydropyrano[2, 3-c]pyrazole derivatives were synthesized and screened for their antimicrobial activity. The precursor, dihydropyrano[2, 3-c]pyrazole was synthesised under catalyst free condition using PEG-400 as reaction medium which facilitated improved yield compared to base catalyzed reaction. Wide scope of substrates, simple workup procedure and high yield even in the absence of catalyst are the major highlights of the protocol. Dihydropyrano[2, 3-c]pyrazoles on condensation with formic acid formed pyrimidine annulated dihydropyrano[2, 3-c]pyrazole derivatives. All the products are characterized using FTIR, $^1H-NMR$ and $^{13}C-NMR$ spectroscopic techniques. The molecules have shown good to moderate activity as antimicrobial agents when compared to the standard drug ciprofloxacin.

The Coordination Chemistry of DNA Nucleosides on Gold Nanoparticles as a Probe by SERS

  • Jang, Nak-Han
    • Bulletin of the Korean Chemical Society
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    • 제23권12호
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    • pp.1790-1800
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    • 2002
  • The DNA nucleosides(dA, dC, dG, dT)bound to gold nanoparticles (~13 nm) in aqueous solution has been studied as a probe by the SERS and their coordination structures have been proposed on the basis of them. According to UV-Visible absorption of gold nanoparticles after modifying with DNA nucleosides, the rates of absorption of dA, dC, and dG were much faster than that of dT as monitored by the aggregation kinetics at 700 nm. These data indicated that the nucleosides dA, dC, and dG had a higher affinity for the gold nanoparticles surface than nucleoside dT. As the result of SERS spectra, the binding modes of each of the nucleosides on gold nanoparticles have been assigned. A dA binds to gold nanoparticles via a N(7) nitrogen atom of the imidazole ring, which the C(6)-$NH_2$ group also participates in the coordination process. In the case of dC, it binds to the gold surface via a N(3) nitrogen atom of the pyrimidine ring with a partial contribution from the oxygen of C(2)=O group. A coordination of dG to the gold surfaces is also proposed. Although the dG has the two different nitrogens of a pyrimidine ring and the amino group, the N(1) nitrogen atom of a pyrimidine ring has a higher affinity after the hydrogen migrates to the amino group. Conversely, dT binds via the oxygen of the C(4)=O group of the pyrimidine ring. Accordingly, these data suggest that the nitrogen atom of the imidazole or the pyrimidine ring in the DNA nucleosides will bind more fast to the gold nanoparticles surfaces than the oxygen atom of the carbonyl group.

Reactions of Pyrimidinonethione Derivatives;Synthesis of 2-Hydrazinopyrimidin-4-one, Pyrimido[1,2-a]-1,2,4-triazine, Triazolo-[1,2-a]pyrimidine, 2-(1-pyrazolo)Pyrimidine and 2-Arylhydrazonopyrimidine Derivatives

  • Attaby, Fawzy-A.;Eldin, Sanaa-M.;Hanafi, Eman-A.Z.
    • 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.

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The Oxidative Iodination of Pyrimidine Bases and their Nucleosides using Iodine/Dimethylformamide/m-Chloroperbenzoic Acid

  • Hwang, Chang-Ho;Park, Jung-Sup;Won, Jeong-Hee;Kim, Jae-Nyoung;Ryu, Eung K.
    • Archives of Pharmacal Research
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    • 제15권1호
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    • pp.69-72
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    • 1992
  • Pyrimidine bases and their mucleosides were oxidatively iodinated at C-5 position by the reaction of iodine in DMF (dimethylformamide) with MCPBA (m-chloroperbenzoic acid) under mild conditions. For uracil derivatives such as uracil 1a. 1, 3-dimethyluracil 1b, uridine 1c, and 2'-deoxyuridine 1d, the corresponding 5-iodo derivatives were obtained in high yields (71-95%). The iodination of cytidine 3a and 2'-deoxycytidine 3b was achieved in moderate yields (41-56%).

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Reactions with Heterocyclic Amidines $(Vl)^1$: Synthesis of some new sym. and assym. pyrazolotriazines and pyrazolo[4,5-e]pyrimidine derivatives

  • Ali Elagamey, Abdel Ghani
    • Archives of Pharmacal Research
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    • 제10권3호
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    • pp.173-178
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    • 1987
  • Several new pyrazolo [1, 5-a]-S-triazine, pyrazolo [4, 5, -elpyrimidine, pyrazolo [1, 5-a] pyrimidine derivatives were synthesized via condensation of 3-antipyrinyl-5-amino-pyrazole (2) with $\beta$$-bifunctional reagents. The azo analogues of pyrazolo [1, 5-a] pyrimidines ; i. e. pyrazolo [5, 1, c]-as-triazine and pyrazolo[5, 1, -c]-as-benzotriazine were synthesized by coupling of diazotized 2-with agents containing active hydrogen.

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Thymidine Production by Corynebacterium ammoniagenes Mutants

  • Song, Kyung-Hwa;Kwon, Do-Young;Kim, Sang-Yong;Lee, Jung-Kul;Hyun, Hyung-Hwan
    • Journal of Microbiology and Biotechnology
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    • 제15권3호
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    • pp.477-483
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    • 2005
  • Corynebacterium ammoniagenes ATCC 6872, which does not accumulate pyrimidine nucleoside or nucleotide, was metabolically engineered to secrete a large amount of thymidine. Characteristics of 5-fluorouracil resistance ($FU^r$), hydroxyurea resistance ($HU^r$), trimethoprim resistance ($TM^r$), thymidylate phosphorylase deficiency ($deoA^-$), inosine auxotrophy ($ino^-$), 5-fluorocytosine resistance ($FC^r$), thymidine kinase deficiency, and thymidine resistance ($thym^r$) were successively introduced into mutant strains KR3 and DY5T9-5, and shake-flask cultures were able to accumulate 408.1 mg/l and 428.2 mg/l of thymidine, respectively, as a major product. The mutant strains did not accumulate thymine at all and accumulated less than 10 mg/l of other pyrimidine nucleosides, such as cytosine, cytidine, and deoxycytidine, as byproducts.

Occurrence of ELISA Inhibitors, and Inhibitor-free Determination of Cyclobutane Pyrimidine Dimers in Japanese Cypress Leaves

  • Hashimoto, Tohru;Nakagawa, Noriko;Okano, Michiaki;Nikaido, Osamu
    • Journal of Photoscience
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    • 제9권2호
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    • pp.448-450
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    • 2002
  • DNA samples extracted from Japanese cypress leaf tissues contain isopropyl alcohol-precipitable, high molecular weight compounds, which interfere ELISA for cyclobutane pyrimidine dimers (CPD). Removal of the compounds is achieved by DEAE ion-exchange column chromatography and improves the ELISA responses of the DNA. When extracting DNA repeatedly from the same leaf tissues, the DNA samples show CPD responses which increase with the order in sequential extraction, and hence for a reliable detennination of DNA lesion a thorough extraction of DNA is required. Clearing these two problems it was demonstrated that CPD level was slightly higher in the leaves of trees growing under full sunlight than in those growing under UBV -cut sunlight.

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Hydrothermal Synthesis, Crystal Structures and Properties of Zinc(II) Di-nuclear Complex and Copper(I) Coordination Polymer Based on Building Block 2-Phenyl-4,6-di(pyridin-2-yl)pyrimidine

  • Zhao, Pusu;Jing, Wang;Jing, Long;Jian, Fangfang;Li, Yufeng
    • Bulletin of the Korean Chemical Society
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    • 제34권12호
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    • pp.3743-3748
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    • 2013
  • A tetradentate ligand of 2-phenyl-4,6-di(pyridin-2-yl)pyrimidine (L) has been synthesized and its complexes with $ZnI_2$ and CuI have been obtained by hydrothermal method. single crystal X-ray diffraction analysis indicates that ligand L coordinates with Zn(II) ions to form a simple four-coordinate di-nuclear complex, while the complexation of L with Cu(I) constructs a one-dimensional chain polymer. The existence of $I^-$ ion hampers the L to assemble grid-type complexes with Zn(II) and Cu(I). Fluorescence spectra show that the L emits blue fluorescence while its Cu(I) polymer decrease the fluorescence intensity and Zn(II) complex quenches the fluorescence.