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Triazolyl Azabicyclo[3.1.0]hexanes: a Class of Potent and Selective Dopamine D3 Receptor Antagonists

✍ Scribed by Giorgio Bonanomi; Simone Braggio; Anna Maria Capelli; Anna Checchia; Romano Di Fabio; Carla Marchioro; Luca Tarsi; Giovanna Tedesco; Silvia Terreni; Angela Worby; Christian Heibreder; Fabrizio Micheli

Publisher: John Wiley and Sons
Year: 2010
Tongue: English
Weight: 613 KB
Volume: 5
Category: Article
ISSN: 1860-7179
DOI: 10.1002/cmdc.201000026

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✦ Synopsis

Abstract

Herein we report a detailed description of the structure–activity relationships for a novel series of “C‐linked” 1,2,4‐triazolylazabicyclo[3.1.0]hexanes. These derivatives are endowed with very high in vitro affinity and selectivity for the dopamine D~3~ receptor. An optimization with respect to undesired affinity toward the hERG potassium channel is also reported. Members of this compound series also show excellent in vitro and in vivo pharmacokinetic properties.

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