title: Ketones as building blocks for dynamic combinatorial libraries: highly active neuraminidase inhibitors generated via selection pressure of the biological target.
abstract: New and potent inhibitors of neuraminidase, a key enzyme in the influenza virus activity, have been discovered in dynamic combinatorial libraries based on ketones and amines as building blocks. Selective synthesis of a number of inhibitors among multiple theoretically possible combinations of building blocks is driven by the presence of the target enzyme.
authors.affiliation: Therascope AG, Im Neuenheimer Feld 584, 69120 Heidelberg, Germany.
authors.forename: Matthias
authors.initials: M
authors.lastname: Hochgürtel
authors.forename: Ralf
authors.initials: R
authors.lastname: Biesinger
authors.forename: Heiko
authors.initials: H
authors.lastname: Kroth
authors.forename: Dorothea
authors.initials: D
authors.lastname: Piecha
authors.forename: Michael W
authors.initials: MW
authors.lastname: Hofmann
authors.forename: Sonja
authors.initials: S
authors.lastname: Krause
authors.forename: Otmar
authors.initials: O
authors.lastname: Schaaf
authors.forename: Claude
authors.initials: C
authors.lastname: Nicolau
authors.forename: Alexey V
authors.initials: AV
authors.lastname: Eliseev
mesh_terms: D000588:Amines / Q000737:chemistry; D020650:Combinatorial Chemistry Techniques; D016208:Databases, Factual; D004791:Enzyme Inhibitors / Q000737:chemistry*; D007659:Ketones / Q000737:chemistry*; D008024:Ligands; D009439:Neuraminidase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D004791:Enzyme Inhibitors; D007659:Ketones; D008024:Ligands; D009439:Neuraminidase