1-Heteroaryl-6-(3,4-dichlorophenyl)-3-azabicyclo[4.1.0]heptane: further insights into a class of triple re-uptake inhibitors |
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Authors: | Micheli Fabrizio Cavanni Paolo Bettati Michela Bonanomi Giorgio Di Fabio Romano Fazzolari Elettra Marchioro Carla Roscic Maja Tarsi Luca Visentini Filippo Zonzini Laura Worby Angela |
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Affiliation: | GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy. fabrizio.micheli@aptuit.com |
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Abstract: | Further exploration around the recently disclosed potent triple re-uptake inhibitor 6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane led to the identification of a new series of potent triple re-uptake inhibitors endowed with good developability characteristics. The insertion of a further aryl moiety into the template allowed the 'titration' of the SERT/NET/DAT ratio leading to the identification of further tools in this important area. |
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