1 research outputs found
1,2,4-Triazolyl 5‑Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists
A novel
series of 1,2,4-triazolyl 5-azaspiro[2.4]heptanes with high affinity
and selectivity at the dopamine (DA) D3 receptor (D3R) is described.
Some of these compounds also have high selectivity over the hERG channel
and were characterized with respect to their pharmacokinetic properties
both in vitro and in vivo during lead identification and early lead
optimization phases. A few derivatives with overall favorable developability
characteristics were selected for further late lead optimization studies