- Synthesis and antibacterial evaluation of 6-azapyrimidines with α-methylene-γ-(4-substituted phenyl)-γ-butyrolactone pharmacophores
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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. Springer Science+Business Media, LLC 2010.
- Huang, Po-Jui,Lee, Kuan-Han
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experimental part
p. 1081 - 1090
(2012/05/05)
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