• 제목/요약/키워드: 2-aminopyrimidine

검색결과 16건 처리시간 0.028초

Synthesis of 2-Thio-4-aminopyrimidine Derivatives as Anti-cancer Agent

  • Lee, Sang-Hyo;Lee, Jin-Ho
    • 대한의생명과학회지
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    • 제15권2호
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    • pp.105-112
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    • 2009
  • The screening of the anti-cancer activity of the chemical library provided 2-thio-4-aminopyrimidine as the initial hit. The confirmation of structure and biological effect of hit was performed by synthesis and biological evaluation. The optimization of hit was performed by derivatization of substituents while keeping the core structure. The evaluation of growth inhibitory activity was carried out using SRB assay against 6 human cancer cell lines and human fibroblast. The growth inhibitory activity of compounds showed substituent dependency and more than 5 compounds showed complete growth inhibition of cancer cell lines at 10 ${\mu}M$ concentration. Chemical library screening followed by synthetic modification provided possibility that 2-thio-4-aminopyrimidine can be used as a new scaffold for the development of anti-cancer agent.

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5-Aminopyrimidine에 대한 아질산의 반응 (Ⅳ) 5-Cyano 및 5-CarboxyPyrimidine 유도체의 합성 (Reaction of Nitrous Acid on 5-Aminopyrimidine (Ⅳ) The Synthesis of 5-Cyano-and 5-Carboxypyrimidines)

  • 장세희;김재순;허태성
    • 대한화학회지
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    • 제13권2호
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    • pp.177-180
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    • 1969
  • 5-Cyanopyrimidine 유도체를 5-Aminopyrimidine 유도체로부터 Sandmeyer반응에 의하여 합성하고 이 화합물들을 가수분해하여 Pyrimidine-5-carbolylic acid 을 합성하였다. 이 방법에 의하면 불순물 제거의 어려움 없이 5-Cyanopyrimidine유도체와 Pyrimidine-5-carboxylic acid유도체를 62%와 65%의 수율로 합성할 수 있었다.

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2-Aminopyrimidine 및 2,4-Dihydoxybenzaldehyde 치환체인 Schiff-염기의 전이금속 착물에 대한 합성 및 특성 그리고 부식방지에의 응용 (Synthesis and Characterization of New Transition Metal Complexes of Schiff-base Derived from 2-Aminopyrimidine and 2,4-Dihydroxybenzaldehyde and Its Applications in Corrosion Inhibition)

  • Ouf, Abd El-Fatah M.;Ali, Mayada S.;Soliman, Mamdouh S.;El-Defrawy, Ahmed M.;Mostafa, Sahar I.
    • 대한화학회지
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    • 제54권4호
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    • pp.402-410
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    • 2010
  • 새로운 착물인 cis-[$Mo_2O_3(Hapdhba)_2$], trans-[$UO_2(Hapdhba)_2$], [Pd(Hapdhba)Cl($H_2O$)], [Pd(bpy)(Hapdhba)]Cl, [Ag(bpy) (Hapdhba)], [$Ru(Hapdhba)_2(H_2O)_2$], [$Rh(Hapdhba)_2Cl(H_2O)$] 및 [Au(Hapdhba)$Cl_2$]를 보고한다. 여기서 $H_2$apdhba는 2-aminopyrimidine 및 2,4-dihydoxybenzaldehyde에서 비롯된 Schiff-염기이다. 이들 착물은 IR, UV-Vis 그리고 질량 스펙트럼을 비롯하여 전기전도도, 자기 및 열 분석을 통해 특성을 조사하였다. 구리의 부식에 대한 $H_2$apdhba의 방해효과는 0.5 M HCl에서 potiodynamic polarization 측정을 통해 조사하였다.

4-아미노피리딘 – HCl, –HBr 복합체에 대한 양자화학적 연구 : 즈비터이온의 안정성 (Stability of the Zwitterionic form of 4-aminopyrimidine HCl and -HBr Complexes: Computational Study)

  • 황태규;박성우;윤영삼;이성렬
    • 대한화학회지
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    • 제53권2호
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    • pp.133-136
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    • 2009
  • 4-아미노피리딘 (4AP)–HCl와 –HBr 복합체에 대한 양자화학적 계산을 수행하였다. 전하분리된 (즈비 터이온) 형태의 [4AP$H^+-Cl^-$]는 안정하지 않으나, [4AP$H^+-Br^-$]은 안정하여 저온기체상에서 관찰될 것으로 예측되었다. 이것은 HCl에 비하여 HBr의 해리에너지가 작다는 사실과, 4AP의 아미노기가 HBr의 “용매”로 작용 한 결과로 해석되었다.

5-Aminopyrimidine에 대한 아질산의 작용 [Ⅱ] Isobarbituric acid의 새 합성법 (Reaction of Nitrous Acid on 5-Aminopyrimidine Derivatives [Ⅱ] Isobarbituric Acid, A New Method of Synthesis)

  • 장세희;김인규;한보섭
    • 대한화학회지
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    • 제9권2호
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    • pp.75-77
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    • 1965
  • 5-Aminouracil을 디아조화한 다음 가수분해시켜 간편하게 isobarbituric acid를 합성하는 새로운 방법을 마련하였다. 이 방법에 따르면 전혀 부반응이 일어나지 않고 대체로 75%이상의 좋은 수율로 isobarbituric acid의 합성이 가능하다.

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Synthesis and Fungitoxicity of Some Pyrimidine Derivatives

  • Ouf, Salama A.;Sherif, Sherif M.
    • Archives of Pharmacal Research
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    • 제16권1호
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    • pp.62-67
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    • 1993
  • A series of 12 pyrimidine derivatives were prepared and tested in vitro against growth, sporulation and nucleic acids of Fusarium oxysporum f. sp. lycopersici and Helminthosporium oryzae. Intorduction of thiazole ring together with two aryl groups to 2-aminopyrimidine induced drastic toxicity for both fungi. Pyrimidine derivatives with aryl groups were less toxic. Nitro groups were found to enhance the toxicity of the pyrimidine derivatives especially when substituted in ortho-position of the aryl groups. Inhibition of nudeic acids synthesis of both fungi was attributed mainly to the presence of thiazole ring.

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항응고성의 2-Chloro-3-(N-Arylamino)-1,4-Naphthoquinone 유도체 합성 (Synthesis of Anticoagulant 2-Chloro-3-(N-Arylamino)-1,4-Naphthoquinones)

  • 유충규
    • 약학회지
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    • 제32권4호
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    • pp.245-250
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    • 1988
  • Naphthoquinone derivatives have been found to be anticoagulant. In this report, several new 2-chloro-3-(N-arylamino)-naphthoquinone derivatives were synthesized in oder to develope mild anticoagulant. 2, 3-dichloro-1, 4-naphthoquinone was reacted with p-aminobenzoic acid, m-aminobenzoic acid, toluidine, m-nitroaniline, sulfanilamide, sulfathiazole, sulfaguanidine, phenetidine, 2-aminopyrimidine and 3-amino-5-methylisoxazole in EtOH or AcOH afford 2-chloro-3-(p-carboxy anilino)-naphthoquinone (1), 2-chloro-3-(m-carboxyanilino)-naphthoquinone (2),2-chloro-3-(toluidino)-naphthoquinone (3),2-chloro-3-(m-nitroanilino)-naphthoquinone (4), 2-chloro-3-(4-sulfanilanilino)-naphthoquinone (5), 2-chloro-3-(4-sulfathiazolino)-naphthoquinone (6),2-chloro-3-(4-sulfaguanidino)-naphthoquinone (7),2-chlro-3-(phenetidino)-naphthoquinone (8), 2-chloro-3-(pyrimidine-2-amino)-naphthoquinone (9) and 2-chloro-3-(5-methylisoxazole-3-amino)-naphthoquinone (10) in good yield.

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Synthesis of Several New Isoxazole, Imidazo[1, 2-a]pyridine, Imidazo[1, 2-a]pyrimidine, Benzoxadiazine and Benzothiazine Derivatives from Hydroximoyl Halides

  • Abdelhamid, Abdou O.;Abdou, Sadek E.;Mahgoub, Sayed A.
    • Archives of Pharmacal Research
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    • 제15권4호
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    • pp.317-321
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    • 1992
  • Furoyldroximoyl chloride 3d reacted with 2-aminopyridine, 2-aminopyrimidine. O-aminophenol, O-phenylenediamine and aminothiophenol to afford imidazo [1, 2-a]pyridine 6. imidazo[1, 2-a]pyrimidine 8, benzoxadiazine 10, nitrosobenzopyrizine 13a and nitrosobenzothiazine 13b, respectively. Isoxazoline 18 and pyrrolidino[3, 4-d]isoxazolin-4, 6-dione derivatives 19a and 19b obtained by the reaction of 3 with acrylonitrile and N-arylmaleimide. Hydroximoyl chloride 3 reacted with thiophenol and sodium benzene-sulfinate to yield furylglyoxaloxime 16a and 16b, respectively. Hydroximoyl chloride 3 reacted also with some active methylene compound to give isoxazole derivatives 20-23, respectively.

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Synthesis of Certain Mercapto and Aminopyrimidine Derivatives as Potential Antimicrobial Agents

  • El-Kerdawy, M.M.;Eisa, H.M.;El-Emam, A.A.;Massoud, M.A.;Nasr, M.N.
    • Archives of Pharmacal Research
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    • 제13권2호
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    • pp.142-146
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    • 1990
  • Reaction of ethyl 4-chloro-2-phenylpyrimidine-4-carboxylate (4) with 5-chloro-2-methylthiophenol or 3-aryl-4-phenyl-1, 2, 4-triazole-5 thiol yielded the corresponding thioethers (5) and (8a, b), respectively. Careful alkaline hydrolysis of (5) yielded the corresponding carboxylic acid (6). Reaction of (4) with p-aminoacetophenone yielded compound (10) which was reacted with certain aromatic aldehyde to afford the$\alpha,\beta$-unsaturated ketones (11a-d). Condensation of (11a-d) with malononitrile or phenylhydrazine yielded the 2-amino-3-cyanopyridines (12a-f) or the 2-pyrazolines (13a, b) respectively. Seven representative compounds were tested for their in vitro antimicrobial activity against some pathogenic micro-organisms, some of them were proved to be active.

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