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    • 13. 发明授权
    • Design, preparation, and properties of antibacterial &bgr;-peptides
    • 抗菌β-肽的设计,制备和性质
    • US06677431B2
    • 2004-01-13
    • US09732911
    • 2000-12-11
    • William F. DeGradoYoshimoto HamuroDahui Liu
    • William F. DeGradoYoshimoto HamuroDahui Liu
    • A61K3804
    • C07C237/12A61K47/56A61K47/6903C07C271/22C07C2603/18
    • An antibacterial &bgr;-peptide having the following formula: wherein R1 is H, an alkyl group including 1-4 carbon atoms, phenyl, heteroaryl, or an alkyl-aryl; R2 is an amine-containing alkyl group having the formula —(CH2)mNH2, wherein m=1, 2, 3, 4, or 5, (CH2)xNHC═NHNH2 wherein x is 1, 2, 3, 4, or 5, a pyridyl, an alkylpryidyl, an amidine-substituted benzyl, a phenyl group, or a cyclic amidine; R3 is H, an alkyl group including 1-4 carbon atoms, phenyl, heteroaryl, or an alkyl-aryl; X is —NH2, —OH, —NHR, or OR where R is alkyl, aryl or acyl groups either free or polymer-supported, a carboxamide, a substituted carboxamide, or a polymer; Y is H, an alkyl group, an acyl group, an acyl-terminated polymer, a sulphonamide, an ether, a urea, a urethane, or a polymer; and n is 2, 3, 4, 5, 6, or 7.
    • 具有下式的抗菌β-肽:其中R 1是H,包含1-4个碳原子的烷基,苯基,杂芳基或烷基 - 芳基; R 2是具有式 - (CH 2)m NH 2的含胺烷基 其中m = 1,2,3,4或5,(CH 2)x NHC = NHNH 2其中x为1,2,3,4或5,吡啶基,烷基基团,脒取代的苄基,苯基 或环状脒; R 3为H,包含1-4个碳原子的烷基,苯基,杂芳基或烷基 - 芳基; X为-NH 2,-OH,-NHR或OR,其中R为烷基,芳基或 Y是H,烷基,酰基,酰基封端的聚合物,磺酰胺,醚,脲,氨基甲酸酯,氨基甲酸酯,氨基甲酸酯, 或聚合物; andn是2,3,4,5,6或7。