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Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and
Laura Bettinetti1, Karin Schlotter, Harald Hübner
1Department of Medicinal Chemistry, Emil Fischer Center, Friedrich-Alexander University, Schuhstrasse 19, D-91052 Erlangen, Germany.
Journal of Medicinal Chemistry
|October 4, 2002
Abstract:
Starting from dopamine receptor ligand BP897, an interactive drug discovery process leading to heterocyclic bioisosteres is demonstrated. The four step strategy involved a careful optimization of geometric and electronic properties by systematic modification of the attachment points and heteroatoms, respectively. Efficacy tuning by modification of the phenyl substituents led to both D3 partial agonists and full antagonists. The benzothiophenes 3c (FAUC346) and 3d (FAUC365) revealed outstanding D3 affinity and subtype selectivity.