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2005
Enzyme inhibiting activity
X 0220
Design of Bivalent Ligands Using Hydrogen Bond Linkers: Synthesis and Evaluof Inhibitors for Human β-Tryptase. — As an alternative to the common
15- 241 ation
approach of covalently linking identical functional groups in a drug molecule, van der
Waals interactions may be involved in constructing a molecular cluster. As compared
to dimers linked by a covalent bond, the pseudo-dimer approach via hydrogen bond
may offer advantages in terms of lower molecule weight, preferable solubility as well
as pharmacokinetic properties. Compounds (I) are tested in a tryptase assay and a preliminary X-ray crystallographic study of the complex between (Ib) and β-tryptase
enzyme confirms the assembly of the expected dimer via hydrogen bonds between the
two molecules, which contribute to the increased potency. — (LI*, Y.; et al.; Bioorg.
Med. Chem. Lett. 14 (2004) 24, 6053-6056; Aventis Pharm., Bridgewater, NJ 08807,
USA; Eng.) — H. Hoennerscheid
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