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Design, synthesis, and activity of novel cis- and trans-3,6-disubstituted pyran biomimetics of 3,6-disubstituted piperidine as potential ligands for the dopamine transporter
- Source :
-
Bioorganic & Medicinal Chemistry Letters . May2003, Vol. 13 Issue 9, p1591. 5p. - Publication Year :
- 2003
-
Abstract
- In our effort to develop novel molecules for the dopamine transporter, we converted our previously designed dopamine transporter specific 3,6-disubstituted piperidine template into corresponding pyran derivatives. cis-Pyran derivative 7b, like their piperidine counterparts, exhibited greater activity for the dopamine transporter compared to the trans-isomer. Further molecular modifications of the cis derivative led to the development of potent analogues which indicated successful bioisosteric replacement of the piperidine ring by a pyran moiety in these 3,6-disubstituted derivatives. [Copyright &y& Elsevier]
- Subjects :
- *DOPAMINE
*PIPERIDINE
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 13
- Issue :
- 9
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 9497285
- Full Text :
- https://doi.org/10.1016/S0960-894X(03)00169-0