Design of bivalent ligands using hydrogen bond linkers: synthesis and evaluation of inhibitors for human β-tryptase

…, J Levell, L Davis, E Albert, M Brollo, A Ugolini…

文献索引：Vaz, Roy J.; Gao, Zhongli; Pribish, James; Chen, Xin; Levell, Julian; Davis, Larry; Albert, Eva; Brollo, Maurice; Ugolini, Antonio; Cramer, Dona M.; Cairns, Jennifer; Sides, Keith; Liu, Feng; Kwong, Jennifer; Kang, Jiesheng; Rebello, Sam; Elliot, Michael; Lim, Hengkeang; Chellaraj, Vinolia; Singleton, Robert W.; Li, Yi Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 24 p. 6053 - 6056

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被引用次数: 13

摘要

We exploit the concept of using hydrogen bonds to link multiple ligands for maintaining simultaneous interactions with polyvalent binding sites. This approach is demonstrated by the syntheses and evaluation of pseudo-bivalent ligands as potent inhibitors of human β- tryptase.