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    Please use this identifier to cite or link to this item: http://ir.cnu.edu.tw/handle/310902800/25389


    標題: Synthesis and antibacterial evaluation of 6-azapyrimidines with α-methylene-γ-(4-substituted phenyl)- γ-butyrolactone pharmacophores
    作者: Huang, Po-Jui
    Lee, Kuan-Han
    貢獻者: 藥物科技研究所
    關鍵字: α-Methylene-γ-butyrolactone
    Antibacterial activity
    Pharmacophore
    Molecular property
    日期: 2011-09
    上傳時間: 2012-06-04 16:40:16 (UTC+8)
    摘要: A series of 6-substituted 2-[(4-methylene-5-oxo-2-(4-substituted phenyl) tetrahydrofuran-2-yl)methyl]-1,2,4-triazine-3,5(2H,4H)-diones (5, 6) and 2,4-bis[(4-methylene-5-oxo-2-(4-substituted phenyl) tetrahydrofuran-2-yl)methyl]-1,2,4-triazine-3,5(2H,4H)-diones (9, 10) were designed, synthesized, and evaluated for antibacterial activity against Gram-positive and Gram-negative microorganisms. The synthesis of these compounds involved the Reformatsky-type reaction between ethyl α-(bromomethyl)acrylate and the proper ketones. Among these compounds, 2-[(4-methylene-5-oxo-2-phenyl tetrahydrofuran-2-yl)methyl]-1,2,4-triazine-3,5(2H,4H)-dione (5a) is the most active compound and shown the selective inhibition activity against Proteus vulgaris.
    關聯: Medicinal Chemistry Research 20(7):p.1081-1090
    Appears in Collections:[藥學系(所)] 期刊論文

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