Ketones as building blocks for dynamic combinatorial libraries: highly active neuraminidase inhibitors generated via selection pressure of the biological target.
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.
Hochgürtel
Matthias
M
Therascope AG, Im Neuenheimer Feld 584, 69120 Heidelberg, Germany.
Biesinger
Ralf
R
Kroth
Heiko
H
Piecha
Dorothea
D
Hofmann
Michael W
MW
Krause
Sonja
S
Schaaf
Otmar
O
Nicolau
Claude
C
Eliseev
Alexey V
AV
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
D000588:Amines; D004791:Enzyme Inhibitors; D007659:Ketones; D008024:Ligands; D009439:Neuraminidase