Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter

Authors
Dutta, AK Davis, MC Reith, MEA
Citation
Ak. Dutta et al., Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter, BIOORG MED, 11(17), 2001, pp. 2337-2340
Citations number
18
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
17
Year of publication
2001
Pages
2337 - 2340
Database
ISI
SICI code
0960-894X(20010903)11:17<2337:RDASON>2.0.ZU;2-E
Abstract
Herein, we report the rational design and synthesis of novel 2,5-disubstitu ted piperidine derivatives in the cis and trans isomeric forms. Out of thes e two isomers, the cis-isomer, 7a, Was found to exhibit the most potent act ivity and selectivity for the dopamine transporter. These novel derivatives represent conformationally constrained version of piperidine analogue of G BR compounds. (C) 2001 Elsevier Science Ltd. All rights reserved.