Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands.
The combination of the 3,5-bis(trifluoromethyl)phenyl group with a spirohydantoin motive as a central scaffold was the basis for the design of a combinatorial library targeted towards the neurokinin-1 receptor. A solution- and solid-phase procedure is described and binding affinities of representative compounds presented.
F. Hoffmann-La Roche AG, Pharma Research, CH-4070, Basel, Switzerland. konrad.bleicher@roche.com
Konrad H
KH
Bleicher
Yves
Y
Wüthrich
Maxime
M
De Boni
Sabine
S
Kolczewski
Torsten
T
Hoffmann
Andrew J
AJ
Sleight
D020650:Combinatorial Chemistry Techniques; D008024:Ligands; D018040:Receptors, Neurokinin-1 / Q000378:metabolism*; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000378:metabolism*
D008024:Ligands; D018040:Receptors, Neurokinin-1; D013141:Spiro Compounds