Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy

  • Bioorg Med Chem Lett. 2002 Feb 25;12(4):633-6. doi: 10.1016/s0960-894x(01)00814-9.
Stefan Löber  1 ,  Tarek Aboul-Fadl ,  Harald Hübner ,  Peter Gmeiner
Affiliations
  • 1. Department of Medicinal Chemistry, Emil Fischer Center, Friedrich-Alexander University, Schuhstrasse 19, D-91052, Erlangen, Germany.
PMID: 11844688 DOI: 10.1016/s0960-894x(01)00814-9
Abstract

Based on the lead molecule FAUC 113, a series of di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives was synthesized and investigated for their Dopamine Receptor binding profile. The carbonitrile 11a (FAUC 327) showed excellent pharmacological properties combining high D4 affinity (K(i)=1.5 nM) and selectivity with significant intrinsic activity (31%) in low nanomolar concentrations (EC50=1.5 nM).