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J Med Chem. 2016 Sep 22;59(18):8549-76. doi: 10.1021/acs.jmedchem.6b00972. Epub 2016 Sep 9.

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.

Author information

1
Aptuit s.r.l. , Via Fleming 4, 37135 Verona, Italy.
2
Dipartimento di Chimica, Università di Parma , Viale delle Scienze, 17/A, Biopharmanet-tec, Viale delle Scienze, 27/A, Campus, I-43124 Parma, Italy.
3
Indivior Inc. , The Fairfax Building, 10710 Midlothian Turnpike, Suite 430, Richmond Virginia 23235, United States.

Abstract

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.

PMID:
27564135
DOI:
10.1021/acs.jmedchem.6b00972
[Indexed for MEDLINE]

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