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…

Index: 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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Citation Number: 13

Abstract

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.