Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter |
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Authors: | Dutta A K Davis M C Reith M E |
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Institution: | Department of Pharmaceutical Sciences, Wayne State University, Detroit, MI 48202, USA. adutta@wizard.pharm.wayne.edu |
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Abstract: | Herein, we report the rational design and synthesis of novel 2,5-disubstituted piperidine derivatives in the cis and trans isomeric forms. Out of these two isomers, the cis-isomer, 7a, was found to exhibit the most potent activity and selectivity for the dopamine transporter. These novel derivatives represent conformationally constrained version of piperidine analogue of GBR compounds. |
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