Synthesis and antibacterial evaluation of 6-azapyrimidines with α-methylene-γ-(4-substituted phenyl)- γ-butyrolactone pharmacophores

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Title:	Synthesis and antibacterial evaluation of 6-azapyrimidines with α-methylene-γ-(4-substituted phenyl)- γ-butyrolactone pharmacophores
Authors:	Huang, Po-Jui Lee, Kuan-Han
Contributors:	藥物科技研究所
Keywords:	α-Methylene-γ-butyrolactone Antibacterial activity Pharmacophore Molecular property
Date:	2011-09
Issue Date:	2012-06-04 16:40:16 (UTC+8)
Abstract:	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.
Relation:	Medicinal Chemistry Research 20(7)：p.1081-1090
Appears in Collections:	[Dept. of Pharmacy] Periodical Articles

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