• Title/Summary/Keyword: Pyrimidines

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Synthesis of Acyclic Nucleosides of 2-Thio-Pyrimidines and -Purines Using a New Coupling Agent of Lithium Bromide

  • Kim, Joong-Young;Kim, Yong-Hae
    • Bulletin of the Korean Chemical Society
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    • v.9 no.5
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    • pp.295-298
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    • 1988
  • Acyclic nucleosides, 1-[[1,3-bis(benzyloxy)-2-propoxy]methyl]-2-thiopyrimidine, 9-[[1,3-bis(benzyloxy)-2-propoxy]methyl]-6-amino -2-thiopurine, 1-(2-acetoxyethoxymethyl)-2-thiopyrimidine, and 9-[[1,3-bis(benzyloxy)-2-propoxy]methyl]-6-amino -2-thiopurine have been synthesized by coupling pyrimidine and purine bases with acyclic acetates using a new coupling reagent of lithium bromide in the presence of trifluoro acetic acid in acetonitrile.

Synthesis and Biological Activities of New Substituted Indoles

  • Hishmat, Orchidee H.;Nakkady, Sally S.;El Shabrawy, Osama A.;Mahmoud, Sawsan S.
    • Archives of Pharmacal Research
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    • v.15 no.1
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    • pp.104-108
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    • 1992
  • 2, 3-Diphenyl-6-formyl-5-methoxyindole reacts with ethyl cyano acetate to yield the arylidene derivative which forms with urea and thiourea the corresponding pyrimidine derivatives. The arylidene derivatives react with hydrazines and with active methylenes to form the respective pyrazole derivatives and the $\alpha, \;\beta$-disubstituted acrylonitriles. Seven new compounds were tested for their effects on the arterial blood pressure of rats and analgesic activity.

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Novel Synthesis of Imidazo[1,2-b]Pyrazoles and Their Fused Derivatives

  • Sherif, Sherif-M.;Hussein, Abdel-HaLeem-M.;El-kholy, Yehya-M.
    • Archives of Pharmacal Research
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    • v.17 no.5
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    • pp.298-303
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    • 1994
  • 4-Arylazo-1H-pyrazol-3, 5-idimines 1a-c reacted with bromomalononitrile (2) to yield the corresponding imidazo[1, 2-b]pyrazoles 3a-c. The latter reacted with some active methylene compounds and with .alpha.-cinnamonitriles to afford the corresponding pyrazoloimidazopyridines 6, 8, 9 and 15, respectively. Compounds 3 reacted with each of formic acid, formamide, trichlo-roacetonitrile and with guanidine to yield the corresponding pyrazoloimidazopyrimidines 16-19 respectively.

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Chemical modifying agents of radiation effect (방사선조사(放射線照射)의 생물학적효과(生物學的效果)에 영향을 미치는 약제(藥劑))

  • Han, Man-Chung;Chang, Kee-Hyun
    • Journal of Radiation Protection and Research
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    • v.5 no.1
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    • pp.32-35
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    • 1980
  • A number of chemical compounds that modify radiation effects are reviewed, with brief report of our own experiments on radioprotective effect of some vasoconstrictive agents and 5-Thio-D-Glucose. Sulfhydryl compounds(-SH group) and some pharmacologic compounds such as CNS depresants, vasoconstrictive agents and autonomic drugs are known to have radioprotective effect in experimental research and in limitted clinical study, whereas oxygen, hallogenated pyrimidines and metronidazole, etc. have radiosensitizing effect. Author experimentally observed some radioprotective effects of angiotensin II, a strong vasoconstrictor, and 5-Thio-D-glucose in mice.

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Reactions of3-Aminopyazole Derivatives with Cyanothioacetamide and Its Derivatives:Synthesis and Reactions of Several New Pyrazole and Pyrazole[3,2-b]Pyrimidine Derivatives

  • Attaby, Fawzy-A.;Eldin, Sanaa-M.
    • Archives of Pharmacal Research
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    • v.20 no.4
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    • pp.330-337
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    • 1997
  • Thiocarboxamidocinnamonitrile derivatives 2 under bar a-f reacted with 3-aminopyrazole derivative 3 under bar a-c to give the pyrazole[3, 2-b]pyrimidine derivatives 6 under bar a-p. Compounds 6 under bar a-p were used as starting material for syntheses of several heterocylic coompounds. Dehydrogenation of 6 under bar gave pyrazole[3, 2-b]pyrimidines 10 under bar a-d while its reaction with diethyl oxalate gave 11 under bar. Reactions of 6 under bar with formic acid gave pyrazolopyrimidines 17 under bar a-j, and pyrazolopyrimidopyrimidines 18 under bar a-j.

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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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    • v.15 no.4
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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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    • v.13 no.2
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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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Synthesis of D-1,3-Dioxolane and L-1,3-Oxathiolane 5-Phenylselenyl Pyrimidine Nucleosides as Potential Antiviral Agents (D-1,3-디옥솔란 및 L-1,3-옥사티올란 5-페닐세레닐 피리미딘 뉴크레오사이드의 합성)

  • Yoo, Jung-Man;Moon, Hyun-Ju;Chung, Byung-Ho;Choi, Bo-Gil;Hong, Joong-Hee;Chun, Moon-Woo
    • YAKHAK HOEJI
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    • v.40 no.1
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    • pp.46-51
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    • 1996
  • Eight new D-1.3-dioxolanyl and L-1,3-oxathiolanyl nucleosides containing 5-phenyl- selenyl pyrimidine bases which are expected to have antiviral activity were synthesized. Condensation of D-1,3-dioxolane acetate and L-1,3-oxathiolane acetate with 5-phenylselenyl pyrimidines gave anomeric mixtures of their nucleosides which were separated by silicagel column chromatography.

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Modeling Aided Lead Design of FAK Inhibitors

  • Madhavan, Thirumurthy
    • Journal of Integrative Natural Science
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    • v.4 no.4
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    • pp.266-272
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    • 2011
  • Focal adhesion kinase (FAK) is a potential target for the treatment of primary cancers as well as prevention of tumor metastasis. To understand the structural and chemical features of FAK inhibitors, we report comparative molecular field analysis (CoMFA) for the series of 7H-pyrrolo(2,3-d)pyrimidines. The CoMFA models showed good correlation between the actual and predicted values for training set molecules. Our results indicated the ligand-based alignment has produced better statistical results for CoMFA ($q^2$ = 0.505, $r^2$ = 0.950). Both models were validated using test set compounds, and gave good predictive values of 0.537. The statistical parameters from the generated 3D-QSAR models were indicated that the data are well fitted and have high predictive ability. The contour map from 3D-QSAR models explains nicely the structure-activity relationships of FAK inhibitors and our results would give proper guidelines to further enhance the activity of novel inhibitors.