| Literature DB >> 26951894 |
Fabrizio Micheli1, Andrea Bernardelli2, Federica Bianchi2, Simone Braggio2, Laura Castelletti2, Palmina Cavallini2, Paolo Cavanni2, Susanna Cremonesi2, Michele Dal Cin2, Aldo Feriani2, Beatrice Oliosi2, Teresa Semeraro2, Luca Tarsi2, Silvia Tomelleri2, Andrea Wong2, Filippo Visentini2, Laura Zonzini2, Christian Heidbreder3.
Abstract
A novel series of 1,2,4-triazolyl octahydropyrrolo[2,3-b]pyrroles showing high affinity and selectivity at the DA D3 receptor is reported here. Compounds endowed with high selectivity over the hERG channel were identified and their pharmacokinetic properties thoroughly analyzed. A few derivatives with appropriate developability characteristics were selected for further studies and progression along the screening cascade. In particular, derivative 60a, (DA D3 pKi=8.4, DA D2 pKi=6.0 and hERG fpKi=5.2) showed a balanced profile and further refinements are in progress around this molecule.Entities:
Keywords: Addiction; Antagonist; DA D3 receptor; Dopamine; Neuroscience
Mesh：
Substances：
Year: 2016 PMID： 26951894 DOI： 10.1016/j.bmc.2016.02.031
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641